Category: benzoxazole

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 general protocol for the N-thioetherification of NH-sulfoximines has been developed. Catalyzed by [Cu(DMAP)4I]I, N-sulfenyl sulfoximines, e.g I, were synthesized by a one-pot cascade reaction with com. available thiophenols as the sulfur source at room temperature The protocol has mild reaction conditions, is operationally simple and affords the corresponding products with good yields and excellent tolerance of functional groups.

A One-Pot Cascade Reaction by Combining NH-Sulfoximines with Thiophenols Under Mild Conditions. 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.

N-Benzylation of NH-sulfoximines via visible light photocatalysis is realized. Under mild reaction conditions, photocatalyst promotes the direct cross-coupling of NH-sulfoximines with benzyl bromides to form N-benzyl sulfoximines. Superbases which are usually used in reported coupling of NH-sulfoximines with alkyl halides were not needed. This method is also suitable for the synthesis of N-allyl sulfoximines.

Photocatalytic N-benzylation of NH-sulfoximines. 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-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.

To assess the potential of N-alkynylated sulfoximines as new (chiral) reagents for organic synthesis, their reactivity profile in numerous synthetic processes is under investigation. When reacted with ketenes, the alkynylated-sulfoximines undergo a 2 + 2|-cycloaddition process to afford sulfoximine-functionalized cyclobutenones in excellent yields.

Exploring the Reactivity of N Alkynylated Sulfoximines: [2 + 2|-Cycloadditions. 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-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.

An efficient synthesis of N-propargylsulfoximines RCCCH(R1)N=S(O)R2R3 [R = C6H5, 4-ClC6H4, (CH2)2C6H5, etc.; R1 = H, C6H5, cyclopentyl, 2H-1,3-benzodioxol-5-yl, etc.; R2 = CH3, C6H5, 2-BrC6H4, etc.; R3 = CH3, C6H5, 4-ClC6H4CH=CH; R2, R3 = -(CH2)4-] was developed through a copper-catalyzed coupling of alkynes RCCH, aldehydes R1CHO and NH-sulfoximines R2R3S(O)NH. The reaction requires no co-catalyst or ligand and shows a wide substrate scope with moderate to good yields.

Synthesis of N-Propargylsulfoximines by Copper-Catalyzed A3-Couplings. 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. 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.

A total of 26 constituents were identified in essential oil from the aerial part. It was found that Haplophyllum latifolium essential oil was a rich source of terpenes. Its composition was dominated by monoterpene (46.1%) and sesquiterpene hydrocarbons (35.5%). The content of oxidized monoterpenes and sesquiterpenes in the essential oil made up on 8.2 and 1.3%, resp. The major constituents of the essential oil were germacrene B (24.7%), limonene (18.2%), ¦Á-phellandrene (14.7%), 3-methyl-2-butenal (6.2%), ¦Â-phellandrene (5.0%), ¦Â-caryophyllene (4.3%), terpinolene (3.9%), ¦Ã-elemene (3.2%), and linalyl acetate (2.6%). The essential oil could be of interest to the perfume and cosmetic industries because of the high content of volatile terpenes and pleasant aroma. Results of the antimicrobial tests showed that S. aureus, B. subtilis, E. coli, and C. albicans were sensitive to the effects of H. latifolium essential oil. The greatest antibacterial effect was found against S. aureus with an inhibition zone diameter of 12.08 ¡À 0.12 mm.

Chemical Composition and Antimicrobial Activity of Essential Oil from the Aerial Part of Haplophyllum latifolium. 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.

An efficient method for the dehydrogenative cross-coupling of dialkyl phosphites with sulfoximines is demonstrated in the presence of copper(II) acetate and triethylamine. A library of sulfoximines including aryl, heteroaryl and alkyl sulfoximines underwent coupling reaction smoothly and gave the desired sulfoximine derived phosphoramidates in good to excellent yields.

Copper-promoted dehydrogenative cross-coupling reaction of dialkyl phosphites with 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-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.

A three component protocol has been developed for the synthesis of N-aroyl sulfoximines by the carbonylation of aryl halides followed by nucleophilic attack of NH-sulfoximines. This reaction tolerates a range of aryl iodides and sulfoximines to provide the N-aroyl sulfoximines in good to excellent yields. Less reactive aryl bromides also underwent sulfoximinocarbonylation and afforded the products. This methodol. is free from phosphine ligands. The heterogeneous Pd/C catalyst was successfully recovered and reused for up to five consecutive catalytic cycles.

Sulfoximinocarbonylation of aryl halides using heterogeneous Pd/C catalyst. 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

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) 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 1621962-30-8.

Typical glucose oxidase (GOx)-based starvation therapy is a promising strategy for tumor treatment; however, it is still difficult to achieve an effective therapeutic effect via a single starvation therapy. Herein, we designed a pH-sensitive polymeric vesicle (PV) self-assembled by histamine-modified chondroitin sulfate (CS-his) for codelivery of GOx and L-buthionine sulfoximine (BSO). GOx can consume glucose to induce the starvation therapy after the PVs reach cancer cell. Moreover, the product H2O2 will be reduced by a high concentration of glutathione (GSH) in the tumor cell, resulting in a reduction of the GSH content. The released BSO finally further reduced the GSH level. As a result, the signaling pathway of the ferroptosis will be activated. The in vivo results demonstrated that GOx/BSO@CS PVs exhibit a good inhibitory effect on the growth of 4T1 tumors in mice. Thus, this work provides a facile strategy to prepare pH-sensitive nanomedicine for synergistic starvation-ferroptosis therapy of tumor.

pH-Sensitive Polymeric Vesicles for GOx/BSO Delivery and Synergetic Starvation-Ferroptosis Therapy of Tumor. 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. 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.

A series of 3-substituted 3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxides was synthesized by condensation of substituted orthanilamides with aldehydes and the compounds tested for their efficacy as diuretic agents. Some side products and unusual reactions which occurred in the application of the general synthetic method were examined The following acetals were prepared by known methods: the diethyl acetals of bromochloroacetaldehyde, iodoacetaldehyde, dibromoacetaldehyde, ¦Á-bromoisovaleraldehyde, ¦Á-bromopropionaldehyde, ¦Á-bromomethylbutyraldehyde, phenylglyoxal, methylthioacetaldehyde, benzylthioacetaldehyde, phenylthioacetaldehyde, phenoxyacetaldehyde, p – chloro-, p-methyl-, and p-methoxyphenylacetaldehydes, and carbethoxyacetaldehyde; the dimethylacetals of ¦Á-bromophenylacetaldehyde and ¦Á-chlorophenylacetaldehyde; and the dipropyl acetal of ¦Á,¦Á-dichloropropionaldehyde. With the exception of p-isopropylphenyl- and 2,4,6-trimethylphenylacetaldehydes, the requisite aldehydes were com. available. The following general methods were used in the condensation of the substituted orthanilamide with various aldehydes. The yields varied from 30 to 90% and optimum conditions were not determined Method A. The substituted orthanilamide (0.01 mole) and 0.2 mole aldehyde component was refluxed 12 hrs. in 25-50 ml. MeCN, the solvent and excess aldehyde evaporated, and the residue crystallized Method B. The orthanilamide and 2 molar equivalents aldehyde (or its acetal) in alc.-HCl were refluxed 1-2 hrs., concentrated, diluted with CHCl3, concentrated, the mixture cooled, the product collected, washed, and recrystallized Method C. The orthanilamide (5 g.), 15-30 ml. acetal, and enough 18% alc.-HCl was heated 30-60 min. at 110-150¡ã, the alc. distilled, the mixture cooled, the solid filtered off, and washed with Et2O. In cases where the product did not crystallize, the excess solvent was removed and the residue triturated with Et2O. Method D. A mixture of the substituted orthanilamide and 1.1 equivalents aldehyde was heated 1 hr. at 200¡ã, cooled, and the crude product recrystallized The following 7-sulfamoyl-dihydrobenzothiadiazine 1,1-dioxides were thus obtained (6-, 5-, 3-substituents, method of preparation, m.p., and recrystallization solvent given): Cl, H, Me, A, 256¡ã, EtOAc-hexane; Cl, Cl, Me, A, 268-9¡ã, EtOAc-hexane; Cl, H, Et, A, 269-70¡ã, tetrahydrofuran-CHCl3; Cl, H, Pr, B, 247¡ã, MeOH-CHCl3; Cl, H, iso-Pr, A, 308-9¡ã, MeCN; Cl, H, Bu, B, 213¡ã, MeOH-CHCl3; CF3, H, Bu, B, 174-5¡ã, EtOAc-CHCl3; Cl, H, iso-Bu, B, 228¡ã, MeOH-CHCl3; Cl, H, tert-Bu, B, 326-7¡ã MeOH; Cl, H, C5H11, B, 207-8¡ã, MeOH-CHCl3; Cl, H, CH2Cl, C, 239-40¡ã, EtOAc-hexane; Cl, H, CH2Br, C, 216-17¡ã EtOAc-hexane; Cl, H, CH2I, C, 214¡ã, EtOAc-hexane; Cl, H, CHBrMe, C, 252-3¡ã, EtOAc-hexane; Cl, H, CHBrPr-iso, C, 180¡ã, EtOAc-hexane; Cl, H, CBrMeEt, C, 188-9¡ã, EtOAc-hexane; Cl, H, CHCl2, B, 280-1¡ã, MeOH-CHCl3; Br, H, CHCl2, B, 264-6¡ã, MeOH-CHCl3; F, H, CHCl2, B, 266¡ã, MeOH-CHCl3; CF3, H, CHCl2, B, 259-60¡ã, MeOH-CHCl3; Cl, H, CHClBr, C, 256¡ã, EtOAc-hexane; Cl, H, CHBr2, C, 247¡ã, EtOAc; Cl, H, CHF2, B, 296-7¡ã, MeOH-CHCl3; Cl, H, CCl2Me, B, 285¡ã, Me2COCHCl3; Cl, H, CMe2CH2OH, B, 250-1¡ã, MeOH; Cl, H, CH2OEt, B, 223¡ã, alc.-CHCl3; Cl, H, CH2COMe, C, 210¡ã, alc.-hexane; Cl, H, glycidyl, A, 246¡ã, MeCN; Cl, H, CH2SMe, B, 216-17¡ã, EtOAc-CHCl3; Cl, H, CH2CO2Et, B, 216-17¡ã, MeOH-CHCl3; Cl, H, CH2NH2, B, 178-80¡ã, Me2CO-pentane; Cl, H, piperidinomethyl, B, 173-5¡ã, EtOAc-hexane; Cl, H, Ph, B, 241-2¡ã, Me2CO-pentane; Cl, H, p-ClC6H4, D, 258-9¡ã, MeOH-CHCl3; Cl, H, o-ClC6H4, D, 272-4¡ã, MeOH-CHCl3; Cl, H, 2,4-(MeO)2C6H3, D, 211-12¡ã, MeOH; Cl, H, 3,4,5-(MeO)3C6H2, B, 244-6¡ã, Me2CO-CHCl3; Cl, H, p-EtO2CC6H4, B, 255-6¡ã, MeOH; Cl, H, p-HO2CC6H4, D, 289-90¡ã, tetrahydrofuran-CHCl3; Cl, H, 2-furyl, B, 190-5¡ã, MeOH-CHCl3; Cl, H, 2-thienyl, D, 211-13¡ã, MeOH-CHCl3; Cl, H, 2-(5-nitrofuryl), B, 239¡ã, MeOH-CHCl3; Cl, H, CH2Ph, C, 267-8¡ã, MeOH; Br, H, CH2Ph, B, 266¡ã, Me2CO-CHCl3; CF3, H, CH2Ph, B, 228¡ã, MeOH-CHCl3; Cl, H, p-MeC6H4CH2, B, 242-4¡ã, MeOH; Cl, H, p-iso-PrC6H4CH2, B, 232-3¡ã, EtOAc-hexane; Cl, H, 2,4,6-Me3C6H2CH2, B, 276-8¡ã, tetrahydrofuran-CHCl3; Cl, H, p-ClC6H4CH2, B, 245-6¡ã, MeOH-Et2O; Cl, H, p-MeOC6H4CH2, B, 239-41¡ã, MeOH; Cl, H, 3,4-(MeO)2C6H3CH2, B, 250-1¡ã, alc.; Cl, H, CHMePh, B, 231-2¡ã, EtOAc-hexane; Cl, H, CH2CH2Ph, B, 230¡ã, MeOH-CHCl3; CF3, H, CH2CH2Ph, B, 234-6¡ã, EtOAc-hexane; Cl, H, (CH2)3Ph, B, 214-15¡ã, MeOH-CHCl3; Cl, H, CH2OPh, B, 257¡ã, Me2CO-CHCl3; Cl, H, CH2SPh, B, 211-13¡ã, MeOH-CHCl3; Cl, H, CH2SCH2Ph, B, 218-19¡ã, MeOH-CHCl3; Cl, H, 3-cyclohexenyl, A, 248-9¡ã, MeOH-CHCl3; Cl, H, Cú·CPh, C, 238-9¡ã, alc.-hexane; Cl, H, 1-(2,5-endo-methylene-3-ethoxycarbonylcyclohexyl), B, 245-7¡ã, MeOH-hexane. HCHO (1.2 g., 36-8%) added to 2.94 g. 5-chloro-2,4-disulfamoylaniline in 5 ml. MeOH, the mixture refluxed 1 hr., evaporated, the residue dissolved in H2O, and cooled gave 2.05 g. 6-chloro-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine, 1,1-dioxide, m. 266.5-7.5¡ã. Essentially the same procedure was used in the preparation of 5,6-dichloro-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 307-9¡ã (H2O), and the 5-methyl-6-chloro analog, m. 302-3¡ã (alc.-H2O). 5-Chloro-2,4-disulfamoylaniline (2.5 g.), 3 g. dichloroacetal, 25 ml. 18% alc.-HCl, and 0.25 ml. H2O refluxed 5 hrs., evaporated, cooled, treated with CHCl3, and refrigerated overnight gave 2 g. 6-chloro-3-dichloromethyl-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide. Difluoroacetic acid (17.9 g.) and 31 g. benzotrichloride containing a little ZnCl2 heated to reflux until HCl evolution ceased and distilled gave 15.6 g. difluoro-N,N-dimethylacetamide (I), b12 101-2¡ã. I (3.1 g.) in 150 ml. Et2O treated in 15 min. with Li diethoxyaluminum hydride in 30 ml. Et2O, the mixture stirred overnight at room temperature, a saturated aqueous solution of 5 ml. Na2SO4 then 70 g. anhydrous Na2SO4 added, the mixture filtered, the ether filtrate added to 25 ml. 4% HCl-alc., and treated with 1 g. 5-chloro-2,4-disulfamoylaniline gave 0.83 g. 6-chloro-3-difluoromethyl-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide. The crude HCl salt (prepared by method C) in 100 ml. hot dilute AcOH filtered, brought to pH 8, and cooled gave 1.1 g. 6-chloro-3,4-dihydro-3-piperidinomethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 173-5¡ã (decomposition). When recrystallized from Me2CO-pentane, a solvate was obtained containing one mole Me2CO. The crude HCl salt of 3-amino-methyl-3,4-dihydro-6-chloro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide in hot H2O cooled, treated with one equivalent aqueous KOH, and cooled gave the free base. 5-Chloro-2,4-disulfamoylaniline (5 g.), 25 ml. chloral, and 5 drops concentrated H2SO4 refluxed 2 hrs., the mixture diluted with CHCl3, and the crude product crystallized gave 2.8 g. 6-chloro-3,4-dihydro-7-sulfamoyl-3-trichloromethyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 301-2¡ã (decomposition) (MeOH-CHCl3). 5-Chloro-2,4-disulfamoylaniline (5 g.), 25 ml. ethoxyacetal, 100 ml. tetrahydrofuran, and 1 ml. 18% alc.-HCl kept 12 hrs. at room temperature gave 0.77 g. 5-chloro-3,4-disulfamoyl-1-(2-ethoxyethylideneamino)benzene, m. 350¡ã (tetrahydrofuran). 5-Chloro-2,4-disulfamoylaniline (2 g.) and 1.98 g. p-CIC6H4CHO heated 0.5 hr. at 230-40¡ã gave 2 products, m. 257-8¡ã and m. 360¡ã, the 1st assigned the structure 6-chloro-3-(p-chlorophenyl)-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide and the 2nd the structure 5-chloro-1-(p-chlorobenzylideneamino)-2,4 -disulfamoylbenzene. 5-Chloro-2,4-disulfamoylaniline (5 g.) and 5.15 g. 3,4,5-trimethoxybenzaldehyde heated 0.5 hr. at 220-5¡ã gave 1.75 g. 5-chloro-2,4-disulfamoyl-1-(3,4,5-trimethoxybenzylideneamino)benzene, m. 300¡ã (MeOH). The same starting material heated 1 hr. with 40 ml. 2% alc.-HCl gave 4.8 g. 6-chloro-3,4-dihydro-7-sulfamoyl-3-(3,4,5-trimethoxyphenyl)-1,2,4-benzothiadiazine 1,1-dioxide, m. 244-6¡ã. Attempted crystallization from MeOH-CHCl3 gave a high yield of starting material. 5-Chloro-2,4-disulfamoylaniline (1 g.) and 0.68 g. o-carboxybenzaldehyde fused 1 hr. at 200-5¡ã gave 0.6 g 5-chloro-1-(2-carboxybenzylideneamino)-2,4-disulfamoylbenzene (II), m. 354¡ã (tetrahydrofuran-CHCl3). The same starting material warmed 1 hr. with 10 ml. 2% alc.-HCl gave 1.35 g. II. 5-Chloro-2,4-disulfamoylaniline (5 g.) heated with 15 ml. BzH gave 7.6 g. crude 7-benzylidenesulfamoyl-6-chloro-3,4-dihydro-3-phenyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 241-2¡ã (Me2CO-pentane). 5-Chloro-2,4-disulfamoylaniline (5 g.), 3.78 g. glycidaldehyde, and 50 ml. 20% alc.-HCl heated 5-10 min., then refluxed 20 min. gave 3.17 g. 6-chloro-3-¦Â-hydroxyethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide (III), m. 320-1¡ã (decomposition) (alc.). 6-Chloro-3-epoxyethyl-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1 – dioxide (0.5 g.) heated 15 min. with 20% alc.-HCl gave 0.42 g. III. 5-Chloro-2,4-disulfamoylaniline (10 g.) and 15 g. dihydroxyacetone in 50 ml. 18% alc.-HCl refluxed 6 hrs., cooled, triturated with Et2O, filtered, and recrystallized gave 12 g. III. 5-Chloro-2,4-disulfamoylaniline (2.8 g.), 1 g. glyceraldehyde, 18 ml. alc., and 12 ml. 30% alc.-HCl refluxed 15 min. gave 1.6 g. III. 5-Chloro-2,4-disulfamoylaniline (4.5 g.), 9 g. phenylglyoxal diethyl acetal, and 70 ml. 8% alc.-HCl heated 2 hrs. gave 2.42 g. 6-chloro-3-(¦Á-hydroxybenzyl) – 7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 282-3¡ã (decomposition). 2,3-Dichloro-4,6-disulfamoylaniline (10 g.) in 800 ml. 95% alc. refluxed overnight with 23 g. 30% aqueous glyoxal gave 2.95 g. 5,6-dichloro-3-hydroxymethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 278-80¡ã (decomposition) (Me2CO). III (5.9 g.) in 250 ml. tetrahydrofuran refluxed 21 hrs. with 5.9 g. NaBH4 gave 1.72 g. 6-chloro-3,4-dihydro-3-¦Â-hydroxyethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 234¡ã (decomposition). An analogous procedure was used for the preparation of 5,6-dichloro-3,4-dihydro-3-hydroxymethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide. 5-Chloro-2,4-disulfamoylaniline (2 g.), 2.8 g. ¦Á-chlorophenylacetaldehyde dimethyl acetal, 100 ml. alc., 40 ml. 23% alc.-HCl, and 3 drops H2O refluxed 1 hr. gave 6-chloro-3-¦Á-chlorobenzyl-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide (IV), m. 182-4¡ã (decomposition), after drying in vacuo m. 198-205¡ã (decomposition). 5-Chloro-2,4-disulfamoylaniline (2 g.), 3.4 g. ¦Á-bromophenylacetaldehyde dimethyl acetal, 100 ml. alc., 40 ml. 23% alc.-HCl, and 3 drops H2O treated as above gave 1.4 g. IV. The ultraviolet absorption spectra were given for a number of the above compounds

3-Substituted dihydrobenzothiadiazine 1,1-dioxides as diuretic agents. 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

(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.

The one-pot synthesis of well-defined 5-(diarylimino) and 5-(sulfoximido)dibenzothiophenium triflates, resp. from diarylimines or sulfoximines, was reported and the structures of a series of these compounds were elucidated by X-ray crystallog. In analogy to their hypervalent I(III) analogs, the iminoyl and sulfoximidoyl groups of these compounds can be selectively transferred to organic substrates. Specifically, the uncatalyzed imination of thiols or sulfinates proceeds with good yields, while under the mild reaction conditions offered by visible light photoredox catalysis, the radical amination of hydrazones or the sulfoximidation of benzylic, allylic and propargylic C-H bonds takes place satisfactorily.

5-(Diarylimino)- and 5-(sulfoximido)dibenzothiophenium triflates: syntheses and applications as electrophilic aminating reagents. 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