Month: December 2022

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

Rosa damascena essential oil (REO) is volatile and unstable. The host-guest complex of beta-cyclodextrin nanoparticles (¦Â-CD) with REO was produced to improve REO characteristics. The REO/¦Â-CD complex was characterized by entrapment efficiency, morphol., crystallinity, particle size, thermal stability, and antioxidant activity. Addnl., the structure of REO/¦Â-CD was evaluated using Fourier transform IR spectroscopy (FT-IR) and NMR (NMR). Results confirmed the formation of REO/¦Â-CD in which the REO, as a guest mol., was entrapped within the ¦Â-CD as a host mol. The encapsulated particles showed a spherical shape with an average diameter of 110 nm and no strong agglomerate. The entrapment of REO within ¦Â-CD led to changes in some physicochem. characteristics and enhancement of the antioxidant activity of REO. Furthermore, beverages with the addition of ¦Â-CD nanoparticle-loaded REO were produced. The beverage containing ¦Â-CD nanoparticle-loaded REO form showed significantly higher overall acceptability than samples containing free REO.

Preparation, characterization, and antioxidant activity of ¦Â-cyclodextrin nanoparticles loaded Rosa damascena essential oil for application in beverage. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

The synthesis of tricyclic dibenzothiazines I (R = 4-FC6H4, 4-H3COC6H4, biphenyl-4-yl, etc.; R1 = H, Me, Br, NO2; R2 = Me, Et) by a ruthenium-catalyzed ortho arylation of Ph sulfoximines with aromatic boronic acids followed by intramol. cyclization in the presence of a palladium catalyst in two consecutive steps were described. Chiral dibenzothiazines II and III were prepared efficiently by using chiral Ph sulfoximine in a similar protocol.

Ruthenium- and palladium-catalyzed consecutive coupling and cyclization of aromatic sulfoximines with phenylboronic acids: an efficient route to dibenzothiazines. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(S-Methylsulfonimidoyl)benzene (BD302898) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 83730-53-4 and 1621962-30-8.

FwThe synthesis of NH-sulfoximines I [R = Ph, Bn, 3-ClC6H4, etc.; R1 = Me, Et, Ph, etc.] from sulfides was developed under mild conditions in an aqueous solution with surfactant TPGS-750-M as catalyst and recyclable hypervalent iodine(III) reagent at room temperature A newly developed hypervalent iodine(III) reagent could readily oxidize sulfides and afforded the corresponding trifluoroiodobenzene, which could be efficiently recovered from the reaction mixture by a simple liquid-liquid biphasic extraction procedure. This protocol was compatible with a broad range of functional groups and could be easily performed on a gram scale, providing a green protocol for the synthesis of compounds I.

Synthesis of NH-Sulfoximines by Using Recyclable Hypervalent Iodine(III) Reagents under Aqueous Micellar Conditions. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

Essential oils (EOs) in vapor phase were applied together with the bacteriocinogenic strain Enterococcus mundtii STw38 to improve the shelf life of Argentinean hake -Merluccius hubbsi-. Evaluated EOs were oregano, thyme, rosemary, and lemongrass. In vitro results demonstrated their effectiveness against foodborne pathogen surrogate Listeria innocua, as well as against Lactobacillus plantarum, Shewanella putrefaciens, and fish indigenous biota. The most effective were oregano and lemongrass, showing the lowest minimal inhibitory concentration, and synergic activity when combined against L. innocua and S. putrefaciens. Furthermore, synergic mixtures promoted changes in target microorganisms cell wall. The composition of the volatile phase of a synergic EOs mixture showed a higher presence of oregano components. When applying the EOs alone in hake fillets, total bacteria count increased 3.3 log cycles whereas in the control system the increase was higher than 5 log cycles, and consumers evaluated similarly in taste and smell both the control and the EOs synergic mixtures When adding the most concentrated synergic mixture (0.147¦ÌL lemongrass/mL headspace and 0.195¦ÌL oregano/mL headspace) together with the bioprotective culture, in 7 days total bacteria count only increased 3 log cycles, showing the effectiveness of the use of EOs together with E. mundtii STw38.

Essential oil in vapor phase in combination with Enterococcus mundtii STw38 to improve refrigerated hake fillets shelf-life. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. The impurity of diuretic hydrochlorothiazide 04, also be a medical intermediate.
2. It’s mainly used for the detection of drug impurities, the synthesis of hydrochlorothiazide and the screening of medical structural fragments.
3. Presents a weak alkaline,refrigeration.

. Recommended Products is: 5250-72-6 and 22503-72-6.

Ring closure of aniline-2,4-disulfonamides with acylating agents, aldehydes, or CO(NH2)2 to give sulfamoylbenzothiadiazine 1,1-dioxide derivatives was described. Sulfamoylbenzothiadiazine 1,1-dioxides promoted excretion of NaCl in animals and man and constituted a novel class of orally effective diuretic agents. Several aspects of the chemistry of this class of compounds were reported in detail. The following procedure was illustrative of the HCO2H ring closure of aniline-2,4-disulfonamides to benzothiadiazine 1,1-dioxides. The yield was typical. 5-Chloro-2,4-disulfamoylaniline (5.7 g.) in 75 ml. 98-100% HCO2H refluxed 24 hrs., the mixture cooled, 100 ml. H2O added, the product collected, washed, and recrystallized gave 6-chloro-7-sulfamoyl-l,2,4-benzothiadiazine 1,1-dioxide (Ia) in 90% yield. 5-Amino-2,4-disulfamoylaniline (1.3 g.) in 20 ml. 98-100% HCO2H refluxed 2.5 hrs. and cooled gave 1.14 g. benzo[1,2-e,5,4-e’]bis-l,2,4-thiadiazine 1,1-dioxide, m. above 500¡ã (HCONMe2). 2-Methylsulfamoylaniline (2 g.) and 5 ml. Et orthoformate heated 0.5 hr. at 125-35¡ã in an open flask, concentrated to dryness in vacuo, and the residue recrystallized gave 1.6 g. 2-methyl-l,2,4-benzothiadiazine 1,1-dioxide (I), needles. Recrystallization of I from 50% hot aqueous alc. gave 2-(N-formyl-N-methylsulfamoyl)aniline, m. 116-18¡ã. Ring closure of 5-chloro-2,4-bis(methylsulfamoyl)aniline was similarly carried out to give 6-chloro-2-methyl-7-methylsulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide; recrystallization from hot aqueous alc. gave 5-chloro-2,4-bis(methylsulfamoyl)-N-formylaniline, plates, m. 192-5¡ã. Ia (15 g.) in 100 ml. Et orthoformate (II) refluxed 24 hrs. and cooled gave 15.4 g. 6-chloro-7-ethoxymethylenesulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide (III), m. 195-6¡ã, resolidified and m. 210-11¡ã (MeCN-Et2O). 6-Chloro-2-methyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide (IV) and II gave 6-chloro-7-ethoxymethylenesulfamoyl-2-methyl-l,2,4-benzothiadiazine 1,1-dioxide, m. 155-7¡ã. Similarly, 6-chloro-7-sulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide and II gave 6-chloro-7-ethoxymethylenesulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide, m. 22-30¡ã (effervescence). NH3 passed into 6.5 g. III in 50 ml. anhydrous alc. 0.5 hr. gave 3.6 g. 7-aminomethylenesulfamoyl-6-chloro-1,2,4-benzothiadiazine 1,1-dioxide, m. 309-11¡ã (alc.). IV similarly treated with NH3 gave 7-aminomethylenesulfamoyl-6-chloro-2-methyl-l,2,4-benzothiadiazine 1,1-dioxide, m. 233-4¡ã. 5-Chloroacetanilide-2,4-disulfonyl chloride (4.4 g.) added por-tionwise to 50 ml. 10% alc.-NH3, the solution evaporated to dryness, and the residue recrystallized from aqueous alc. gave 6-chloro-3-methyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide. Similarly, with concentrated NH4OH 6-chloro-3-propyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide and 3-amyl-6-chloro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide were prepared from the corresponding N-acylanilinedisulfonyl chlorides. 5-Chloro-2,4-disulfamoyl-N-(chloroacetyl)aniline (7.2 g.) in 30 ml. HCONMe2 heated 1.5 hrs. with 2.3 g. anhydrous KF, cooled, and diluted with H2O gave 5.5 g. 3-chloromethyl-6-chloro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide. Method (A). 5-Chloroaniline-2,4-disulfonyl chloride (7.2 g.) in 13 ml. BzCl left overnight at room temperature gave 10.9 g. 5-chloro-N-benzoylaniline-2,4-disulfonyl chloride, which washed and heated 2 hrs. on the steam bath with C6H6 and 50 ml. concentrated NH4OH gave 2.7 g. 6-chloro-3-phenyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide (V), needles. Acidification of the ammoniacal filtrate gave 5-chloro-2,4-disulfamoyl-N-benzoylaniline (VI). Method (B). VI (1 g.) in 25 ml. concentrated NH4OH left 48 hrs. at room temperature gave 84% V. In like manner, ring closure of 5-chloro-2,4-disulfamoyl-N-(p-chlorobenzoyl)aniline gave 85% 3-(p-chlorophenyl)-6-chloro-7-sulfamoyl-l,2,4-benzothiadiazine 1,1-dioxide. 5-Chloro-2,4-disulfamoyl-N-(o-chlorobenzoyl)aniline similarly afforded 56% 3-(o-chlorophenyl)-6-chloro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide. The following substituted 1,2,4-benzothiadiazine 1,1-dioxides were obtained (substituents at 2, 3, 5, 6, and 7, recrystallization solvent, and m.p. given): H, H, H, H, SO2NH2, alc.-H2O, 319-20¡ã; H, H, H, F, SO2NH2, alc.-H2O, 304-5¡ã; H, H, H, Cl, SO2NH2, alc.-H2O, 342.5-3.0¡ã; H, H, H, Br, SO2NH2, HCONMe2-H2O, 347-9¡ã; H, H, H, CF3, SO2NH2, alc.-hexane, 294-5¡ã; H, H, H, Me, SO2NH2, AcOH-H2O, 344-5¡ã; H, H, H, OMe, SO2NH2, alc.-H2O, 305-7¡ã; H, H, H, NO2, SO2NH2, alc.-H2O, 338-9¡ã; H, H, H, NH2, SO2NH2, alc.-H2O, 323-4¡ã; Me, H, H, Cl, SO2NH2, HCONMe2-Et2O, 217-20¡ã; H, Me, H, Cl, SO2NH2, alc., 332¡ã; H, Pr, H, Cl, SO2NH2, alc.-H2O, 305-7¡ã; H, C5H11, H, Cl, SO2NH2, alc.-H2O, 269-70¡ã; H, ClCH2, H, Cl, SO2NH2, alc.-H2O, 323-6¡ã; H, Ph, H, Cl, SO2NH2, HCONMe2-H2O, above 350¡ã; H, o-ClC6H4, H, Cl, SO2NH2, alc.-H2O, above 350¡ã, H, p-ClC6H4, H, Cl, SO2NH2, alc.-H2O, above 350¡ã; H, H, Cl, H, SO2NH2, alc.-H2O, 276.5-7.5¡ã; H, H, Cl, Cl, SO2NH2, alc.-H2O, 355-6¡ã; H, H, I, Cl, SO2NH2, HCONMe2H2O, 276-7¡ã; Me, H, H, Cl, SO2NHMe, alc., 219-21¡ã; p-ClC6H4, H, H, Cl, SO2NHC6H4Cl-p, MeCN, 247-9¡ã; H, H, H, Cl, SO2NMe2, alc.-H2O, 265-7¡ã; H, H, SO2NH2, H, H, Me2CO-C6H6, 249-50¡ã; H, H, SO2NH2, H, Br, Me2CO, 291-2¡ã; H, H, SO2NH2, H, SO2NH2, alc.-H2O, 316-18¡ã; H, H, H, SO2NH2, H, alc.-H2O, 309-12¡ã; H, H, H, SO2NH2, Cl, Me2CO-ligroine, 327-30¡ã; H, H, H, Cl, H, butanone, 253-4¡ã; H, H, H, Cl, Cl, Me2CO-ligroine, 293-4¡ã; H, H, H, Cl, Me, alc.-H2O, 287-8¡ã; H, H, H, Me, Cl, MeCN, 260-1¡ã; H, H, H, Cl, MeSO2, alc.-H2O, 329-31¡ã; Me, H, H, H, H, alc., 95-7¡ã. The general procedure for the preparation of 3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxides. Method (A). The orthanilamide compound (0.02 mole) and 0.025 mole of 37% HCHO in 50 ml. 90% alc.-H2O containing 300 mg. NaOH heated 2 hrs. on the steam bath, acidified, and the mixture cooled gave 80% yield. Method (B): acid catalyzed ring closure. The orthanilamide compound (0.02 mole) and 0.04 mole paraformaldehyde in 60 ml. alc. and 60 ml. 6N HCl heated and after 1 hr. the product isolated gave an average yield of 85-90%. The following substituted 3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxides were thus obtained (substituents at 5 and 6 and m.p. given): H, H, 216-17¡ã; H, Cl, 262-3¡ã; H, Br, 287-8¡ã; H, CF3, 263-4¡ã; H, Me, 253-4¡ã; H, NO2, 263.5-4.5¡ã; Cl, Cl, 288-9¡ã. Likewise the following 6-chloro-substituted 3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxides were obtained (substituents at 2, 4, and 7, m.p., and recrystallization solvent given): H, H, H, 164-6¡ã, PhMe; H, Me, SO2NH2, 249-50¡ã, alc.-H2O; Me, H, SO2NH2, 239-41¡ã, alc.-H2O; Me, H, SO2NHMe, 195-7¡ã, alc.; H, H, SO2NMe2, 202-4¡ã, alc.-H2O; H, H, MeSO2, 248-9¡ã, alc.-H2O. The following 6-chloro-7-sulfamoyl-3,4-dihydro-2-substituted-1,2,4-benzothiadiazine 1,1-dioxides were obtained by ring closure of 5-chloro-2,4-disulfamoylaniline with the appropriate aldehyde. Acid cyclization was used for compounds number 1, 2, and 9, and base cyclization for the remainder (compound number, 2-substituent, m.p., and recrystallization solvent given): 1, Me, 252-3¡ã, AcOH-H2O; 2, Et, 265¡ã, AcOH-H2O; 3, CCl3, 287¡ã, ethylene glycol monomethyl ether-H2O; 4, CH2OH, 225-6¡ã, Me2CO-H2O; 5, oxiranyl, 233-5¡ã, Me2CO-H2O; 6, (CH2)5, 259-60¡ã, HCONMe2-H2O; 7, PhCH2, 260-2¡ã, AcOH-H2O; 8, p-ClC6H4, 250-1¡ã, AcOH-H2O; 9, p-O2NC6H4, 268-9¡ã, Me2CO-Et2O; 10, 2-pyridyl, 260¡ã, MeCN; 11, 5-nitro-2-furyl, 239-40¡ã, Me2CO-Et2O. 5-Chloro-2,4-disulfamoylaniline (11.4 g.) in 20 ml. HCONMe2 and 17.6 g. CCl3CHO heated 24 hrs. on the steam bath, 100 ml. H2O added, and the solid reprecipitated from dilute NH4OH gave 14.5 g. 6-chloro-7-sulfamoyl-3-trichloromethyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide. When the reaction was carried out in 60 ml. HCONMe2 in the presence of 4.6 g. anhydrous KF 3 hrs. on the steam bath, 76% 6-chloro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 330¡ã, was isolated, ¦Ë 225 and 279-80 m¦Ì, ¦Å 29,592 and 11,465. 5-Chloro-2,4-disulfamoylaniline (5.7 g.) and 5.9 g. cyclohexanone in 30 ml. HCONMe2 heated 2 hrs. with 2.3 g. anhydrous KF gave 7 g. 6-chloro-7-sulfamoyl-3,3-pentamethylene-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide. The following was illustrative of the method used for preparation of 3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxides. Compounds were recrystallized from aqueous alc. in yields of 35-73%. 5-Chloro-2,4-disulfamoylaniline (8.4 g.) and 3.5 g. CO(NH2)2 was heated 45-60 min. at 200¡ã (NH3 evolved), the solid cooled, dissolved in H2O, filtered, acidified, and recrystallized from aqueous alc. The following compounds were thus obtained (substituents at 4, 5, 6, 7, and m.p. given): H, H, Cl, SO2NH2, 313¡ã; H, Cl, H, SO2NH2, 314-15¡ã; H, H, SO2NH2, Cl, 323-4¡ã; H, H, Br, SO2NH2, 323-4¡ã; H, H, Me, SO2NH2, 307-8¡ã; H, H, MeO, SO2NH2, 291-3¡ã; H, H, NO2, SO2NH2, above 350¡ã; Me, H, Cl, SO2NH2, 315¡ã. Ia (5.9 g.) in 25 ml. H2O containing 0.88 g. NaOH shaken 10 min. with 3 g. Me2SO4 at room temperature, the precipitate collected, washed, dried, and crystallized gave 2.8 g. 6-chloro-4-methyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide (VII), m. 325-6¡ã (Me2CO-alc.). VII heated 2.5 hrs. with 10% NaOH gave 5-chloro-2,4-disulfamoyl-N-methylaniline (VIII). Method (B). VIII (5 g.) in 70 ml. 98-100% HCO2H refluxed 24 hrs. and cooled to room temperature gave 4.7 g. VII. Ia (32.2 g.) added portionwise to 2.5 g. Na in 200 ml. alc., 16.3 g. CH2:CHCH2Br added, the solution warmed 24 hrs. with intermittent addition of 4 g. CH2:CHCH2Br after 6 hrs., and cooled gave 27.2 g. solids. Repeated extraction of this solid with Me2CO at room temperature gave 11.9 g. unchanged Ia and 12.5 g. 4-allyl-6-chloro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide (IX), m. 243-5¡ã (aqueous alc.). IX (1 g.) in 20 ml. 10% NaOH heated 2 hrs. gave 0.5 g. 5-chloro-2,4-disulfamoyl-N-allylaniline (IXa), m. 181-3¡ã (H2O). IX (1 g.) in 70 ml. H2O and 9 ml. N NaOH left 0.5 hr. at room temperature, cooled, acidified, and the precipitate collected gave 0.4 g. 5-chloro-2-formylsulfamoyl-4-sulfamoyl-N-allylaniline (X), needles, m. 142.5-3.5¡ã (CHCl3-Me2CO). Recrystallization of X from H2O gave IXa. 3,4-Dimethyl-1,2,4-benzothiadiazine 1,1-dioxide (11.4 g.) in 35 ml. ClSO3H heated 2.5 hrs. at 150-60¡ã, poured onto ice, the solid added to 50 ml. concentrated NH4OH, after 30-60 min. the product collected, and recrystallized gave 3,4-dimethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 258-60¡ã (HCONMe2-alc.). Reprecipitation of a sample from dilute NaOH gave 2-acetylsulfamoyl-4-sulfamoyl-N-methylaniline, m. 208-10¡ã (Me2CO-ligroine). Ac2O (25 ml.) left overnight at room temperature with 8.9 g. Ia in 75 ml. C5H5N, the product collected, and dried gave 7.7 g. 7-acetylsulfamoyl-6-chloro-1,2,4-benzothiadiazine 1,1-dioxide (XI), m. 299¡ã (rapid heating), pK’a 3.7, 7.2. XI (2 g.) in 10 ml. 10% NaOH heated 15 min., cooled, and acidified gave 4-acetylsulfamoyl-5-chloro-2-sulfamoylaniline (XII), plates, m. 221¡ã (Me2CO-alc.). Cyclization of XII with HCO2H gave 7-acetylsulfamoyl-6-chloro-1,2,4-benzothiadiazine 1,1-dioxide. Butyric anhydride (25 ml.) left at room temperature overnight with 8.9 g. Ia in 75 ml. C5H5N, poured into ice H2O, and acidified gave 8.1 g. 7-butyrylsulfamoyl-6-chloro-1,2,4-benzothiadiazine 1,1-dioxide, m. 286¡ã (alc.-H2O). Ia (10 g.) left 2 hrs. at room temperature with 50 ml. NHMe2, dissolved in 50 ml. 50% aqueous alc., and acidified gave 5.8 g. 5-chloro-2-dimethylaminomethylenesulfamoyl-4-sulfamoylaniline, m. 208-10¡ã (alc.-H2O). Ia (10 g.) and 13.6 g. piperidine heated 1 hr. on the steam bath, diluted with H2O, and acidified gave 3.8 g. 5-chloro-2-piperidinomethylenesulfamoyl-4-sulfamoylaniline, m. 210-12¡ã (aqueous alc.). Ia (29.6 g.) added portionwise to 150 ml. ClSO3H, the mixture heated 2 hrs. on the steam bath, cooled, poured onto crushed ice, and the solid collected gave 30.3 g. 6-chloro-1,2,4-benzothiadiazine-7-sulfonyl chloride 1,1-dioxide (XIIa), m. 259-61¡ã (Me2CO-hexane). 6-Chloro-2-methyl-7-methylsulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide (68.3 g.) added portionwise to 200 ml. ClSO3H, the mixture heated 5 hrs., cooled, poured onto ice, and collected gave 60 g. 5-chloro-2-methylsulfamoylaniline-4-sulfonyl chloride (XIII), m. 158¡ã (effervescence) (Me2CO-C6H6). XIII (43.2 g.) added portionwise to 250 ml. concentrated NH4OH, the mixture heated 1 hr., concentrated, and the solid recrystallized gave 17.9 g. 5-chloro-2-methylsulfamoyl-4-sulfamoylaniline as 2 crystal modifications, m. 168-70¡ã and 188-90¡ã. XIIa (10 g.) added to 30 ml. MeNH2 and left at room temperature gave a residue, which dissolved in 200 ml. 5% NaOH, heated 2 hrs., and acidified gave 6.4 g. 5-chloro-4-methylsulfamoyl-2-sulfamoylaniline, m. 182-3¡ã (H2O). XIIa (30 g.) left at room temperature with 150 ml. anhydrous NHMe2 gave 22.8 g. 5-chloro-2-dimethylaminomethylenesulfamoyl-4-dimethylsulfamoylaniline (XIV), m. 195-7¡ã (alc.). XIV (6.7 g.) in 20 ml. 10% NaOH heated 1 hr. and acidified gave 4.0 g. 5-chloro-4-dimethylsulfamoyl-2-sulfamoylaniline, m. 158-60¡ã (aqueous alc.). Ia (3 g.) in 100 ml. MeOH reduced at room temperature and 39 lb./sq. in. initial H pressure over 1 g. 5% ruthenium-C, after 10 hrs. the mixture heated, filtered, and concentrated gave 83% 6-chloro-7-sulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide (XV). KMnO4 (3.75 g.) added portionwise to 8.9 g. XV in 150 ml. H2O and 10 ml. 20% NaOH, the solution stirred 15 min. at room temperature, warmed 5 min. on the steam bath, excess KMnO4 destroyed with 2-3 ml. alc., and the solution acidified gave 7.4 g. 6-chloro-7-sulfamoyl-1,2,4-benzothiadiazine. Similar oxidation of 6-methyl-7-sulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide gave a comparable yield of 6-methyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 345¡ã. 5-Chloro-2,4-bis(dimethylsulfamoyl)aniline (XVI) (3.4 g.) and 10 g. 50% PhCH2CHO in alc. heated 0.5 hr. at 150¡ã, the mixture cooled, and the solid triturated with MeCN gave 2.4 g. 5-chloro-2,4-bis(dimethylsulfamoyl)-N-(2-phenylethylidene)aniline, m. 203-5¡ã (MeCN), ¦Ë 226-8 and 337-40 m¦Ì, ¦Å 27,351 and 36,106. XVI (3.4 g.), 3 g. p-O2NC6H4CHO, and 60 ml. PhMe refluxed 20 hrs., cooled, and the solid triturated with 200 ml. refluxing alc. gave 3.6 g. 5-chloro-2,4-bis(dimethylsulfamoyl)-N-(p-nitrobenzylidene)aniline, m. 221-3¡ã (MeCN), ¦Ë 276-281 m¦Ì, ¦Å 25,270. The ultraviolet absorption spectra were given for a number of 1,2,4-benzothiadiazine 1,1-dioxides and 5-chloro-2,4-disulfamoylanilines.

Diuretics: 1,2,4-benzothiadiazine 1,1-dioxides. Recommended basis is hydrochlorothiazide 20. Products is: https://www.ambeed.com/products/742-20-1.html, 432499-63-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

Copper-mediated cross-coupling reactions of sulfoximines with aryl iodides and aryl bromides provide N-arylated sulfoximines in high yields. The method is complementary to the known palladium-catalyzed N-arylation and allows the preparation of N-arylated sulfoximines, which have previously been inaccessible.

Copper-Mediated Cross-Coupling Reactions of N-Unsubstituted Sulfoximines and Aryl Halides. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

Rhodium-catalyzed directed CH-functionalizations have been used in hydroarylations of heterobicyclic alkenes with NH-sulfoximines. Unexpectedly, the bicyclic framework is retained, resulting in the formation of addition products being attractive intermediates for functionalized mols. that are difficult to prepare by other means.

Hydroarylations of Heterobicyclic Alkenes through Rhodium-Catalyzed Directed C-H Functionalizations of S-Aryl Sulfoximines. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

Schinus terebinthifolia Raddi (Anacardiaceae) is rich in essential oil, distinguished by a predominance of monoterpenes and sesquiterpenes, it being widely used in traditional medicine for the treatment of inflammations. This study¡äs objective was to investigate the chem. composition of the essential oil of S. terebinthifolia (EOST) collected in six states of Brazil, evaluate its anti-inflammatory effects in mice, and analyze the histochem. and micromorphol. of leaves and stems.Aerial parts of S. terebinthifolia were collected in six states of Brazil, and the essential oil was extracted by hydrodistillation and analyzed by gas chromatog.-mass spectrometry (GC-MS). The histochem. and micromorphol. of leaves and stems were performed using standard reagents, light and field emission SEM, beyond energy-dispersive X-ray spectroscopy. The EOST were evaluated for anti-inflammatory activity and hyperalgesia using the carrageenan-induced paw edema methodol. The EOST showed variation across the six states in its yield (0.40%-0.86%) and chem. composition: hydrocarbon monoterpenes (28.76%-47.73%), sesquiterpenes, (31.43%-41.76%), oxygenated monoterpenes (14.31%-19.57%), and oxygenated sesquiterpenes (4.87%-14.38%). Both ¦Á-pinene and limonene were predominant constituents of essential in five regions, except for one state where ¦Á-phellandrene and limonene were the dominant components. A comprehensive description of the leaf and stem micromorphol. and histochem. was performed. In the in vivo testing, all EOST samples exerted antiedematogenic and anti-hyperalgesic effects, when tested in a carrageenan-induced paw inflammation (mech. and thermal hyperalgesia) model with oral doses of 30 mg/kg. Our results indicate that the EOST samples collected in six Brazilian states differed in their chem. composition but not their anti-inflammatory and antihyperalgesic effects, which was correlated with the synergistic effect of its components, collaborating the etnhopharmacologycal use of this plant due to its an anti-inflammatory effect. Also, micromorphol. and histochem. of leaves and stems presented in this study provide anatomical and microchem. information, which aids species identification.

Geographical variation in the chemical composition, anti-inflammatory activity of the essential oil, micromorphology and histochemistry of Schinus terebinthifolia Raddi. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Iminotetrahydrothiophene 1-oxide (BD00963737) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

A copper(I)-catalyzed three-component reaction of alkynes RCCH (R = C6H5, biphenyl-4-yl, naphthalen-1-yl, etc.), sulfoximines R1(R2)S(=NH)(O) [R1R2 = -(CH2)4-; R1 = C6H5, 4-FC6H4, 4-ClC6H4, 4-NCC6H4; R2 = CH3, CH2CH3] and azides R3N3 [R3 = 4-BrC6H4CH2, cyclohexyl, 2-(naphthalen-1-yl)ethyl, etc.] is described. This reaction proceeds under mild conditions with copper salt as a catalyst and atm. oxygen as an oxidant to afford a variety of 1,2,3-triazolyl-5-sulfoximines I in moderate to good yields.

Synthesis of fully-substituted 1,2,3-triazoles via copper(I)-catalyzed three-component coupling of sulfoximines, alkynes and azides. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Iminotetrahydrothiophene 1-oxide (BD00963737) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

The Rh(II)-catalyzed imination of sulfoxides and sulfides using [Rh2(OAc)4] as a catalyst and trifluoroacetamide or sulfonylamides in combination with iodobenzene diacetate and magnesium oxide affords sulfoximines and sulfilimines, resp., in a stereospecific manner.

Rhodium-Catalyzed Imination of Sulfoxides and Sulfides: Efficient Preparation of N-Unsubstituted Sulfoximines and Sulfilimines. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem