Day: December 1, 2022

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 novel rhodium-catalyzed imination of sulfoxides using O-(2,4-dinitrophenyl)hydroxylamine is developed under mild conditions with good functional group tolerance. This method provides an efficient access to free NH-sulfoximines, an important structural unit in a variety of biol. active compounds E.g., in presence of Rh2(esp)2 and O-(2,4-dinitrophenyl)hydroxylamine in trifluoroethanol, imination of sulfoxide derivative (I) gave 84% sulfoximine derivative (II).

Rhodium-catalyzed direct synthesis of unprotected NH-sulfoximines from sulfoxides. 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

(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.

This study was conducted to construct a multifunctional nanodrug delivery system (NDDS) to deplete glutathione (GSH) in tumor cells and amplify oxidative stress, enhancing the synergistic effect of chemotherapy and photodynamic therapy (PDT). L-Buthionine-sulfoximine (BSO) and chlorin e6 (Ce6) were loaded into mesoporous silicon nanoparticles (MSN), and then MSN were modified with oxidized hyaluronic acid (OHA) as a pore-blocking agent. Cisplatin (Pt(II)) was further loaded by a coordination reaction with carboxyl groups in OHA to yield a multifunctional NDDS (denoted as MSN@OHA-Ce6/BSO/Pt). The physicochem. properties and antitumor activity of the prepared nanoparticles were characterized in detail. In vitro and in vivo experiments demonstrated that OHA was shed from MSN@OHA-Ce6/BSO/Pt under acidic conditions in tumors, resulting in the release of free BSO, Ce6, and Pt(II). The released BSO could reduce intracellular GSH expression by 48.8%, effectively enhancing the PDT effect of Ce6 and the chemotherapy effect of Pt(II). Finally, the tumor inhibitory rate (vs saline) reached 73.8% ¡À 2.5% for MSN@OHA-Ce6/BSO/Pt in A549/DDP tumor-bearing nude mice. Therefore, the multifunctional NDDS significantly enhanced the synergistic effect of PDT and chemotherapy.

Construction of multifunctional mesoporous silicon nano-drug delivery system and study of dual sensitization of chemo-photodynamic therapy in vitro and in vivo. 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.

cf. ibid. 25,229(1962). On the basis of testing 15 sulfonamide derivatives for diuretic action in rats, 6 compounds [4 highly active: hydrochlorothiazide(HCT), 5-chlorohydrochlorothiazide(HCT-55), benzthiazide(CT-S), and 3-diethylaminomethylhydrochlorothiazide(HCT-16); one moderately active: chlorothiazide(CT); and one inactive: 3-(3,4-dimethoxy-2-ethoxycarbonylphenyl)hydrochlorothiazide(HCT-18)] were chosen for comparative study on physiol. disposition in rats. A modification of the method of Baer, et al. (CA 53, 11639f) was used for the determination of these compounds in biol. materials. After an oral dose of 20 mg./kg., the rate of disappearance of the various compounds from the gastrointestinal tract was found to follow the decreasing order of HCT-55, CT-S, HCT-16, HCT, CT, and HCT-18. This order roughly parallels their oil-water partition coefficients with the exception of HCT-18, which was found to have the highest partition coefficient, although absorbed rather slowly. CT was demonstrated to have the lowest partition coefficient, which may explain its relatively slow rate of absorption from gastrointestinal epithelium. In addition, its low pKa value (the pKa1 of CT was found to be 6.7, while those of all other compounds investigated were between 9.0-9.2) may also affect its rate of absorption. For all compounds given orally, the highest concentrations were found in the kidneys, though three patterns of tissue distribution were observed. CT, HCT, and HCT-55 were all characterized by a specific affinity for the kidney tissue and very low levels in other organs; DSA was distributed rather nonspecifically in various tissues; while for CT-S and HCT-16, equally high levels were found both in the kidneys and in the liver. When given orally, the rate of excretion of the compounds in the urine was found to be essentially parallel to the rapidity of disappearance from the gastrointestinal tract, i.e., HCT-55 > CT-S > HCT > HCT-16 > CT. After intravenous injection, nearly all of the administered dose of CT-S and HCT was found in the first five-hr. urine. The percentages of urinary excretion of HCT-55, HCT-16, CT, DSA, and HCT-18 were 92, 84, 79, 58, and 29%, resp. The possible relation between the characteristics of the renal transport of these compounds and their diuretic potencies are discussed in some detail.

Oral diuretics. III. Characteristics of the dispositions of some sulfonamide diuretics and their relations to diuretic actions. 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.

Visible light induces C-C-bond cleavage reactions of ketones, which can be utilized for N-acylations of sulfoximines. No (photo)catalyst is required, and the reactions occur at ambient temperature in air. The substrate scope is broad for both ketones and sulfoximines. For converting NH-sulfoximines, the presence of NBS is essential.

Visible light-induced C-C bond cleavage in a multicomponent reaction cascade allowing acylations of sulfoximines with ketones. 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

(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.

Direct difunctionalization of chem. distinct ortho- and peri-C-H bonds of fused hetero(arenes) was illustrated through an unusual one-pot domino {[4 + 2] and [5 + 2]} double annulation with alkynes for the first time. This process was viable under Ru(II)-catalysis using a sulfoximine directing group and builds four bonds [(C-C)-(C-N) and (C-C)-(C-O)] in a single operation. Such synthetic manifestation offers access to uncommon [6,7]-fused oxepino-pyridine skeletons, e.g., I. DFT calculations provided mechanistic insight into this double annulation of naphthoic acid derivatives with alkynes and corroborate the participation of a ruthena-oxabicyclooctene intermediate, which was responsible for the rare 7-membered ring formation.

Double annulation of ortho- and peri-C-H bonds of fused (hetero)arenes to unusual oxepino-pyridines. 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.

In this study, the effect of starch-based and gelatine-based edible coating containing cinnamon oil on selected quality parameters and the metabolism of antioxidants in highbush blueberry fruit, in terms of extending their shelf life were investigated. Research showed that the application of cinnamon oil to edible coating pos. influenced the quality of the fruit during storage. Coating with essential oil effectively inhibited the growth of yeast and mold in the fruit during storage. On the last day, the growth of yeast and mold in the fruit coated with cinnamon oil (10% COE) was 1.29 log cycles lower than in the control. Moreover, the essential oil reduced the loss of soluble solids but it did not significantly affect the acidity and weight loss of the fruit. Equally interesting was the effect of the coating with cinnamon oil on the antioxidant activity of the fruit. Blueberries coated with cinnamon oil were characterised by a lower ability to produce ROS, as well as a lower activity of antioxidant enzymes. On the final day, the level of ROS and the activity of SOD and CAT were lower than the control by 82%, 56% and 63% resp. The level of polyphenols in the fruit coated with cinnamon oil was higher than in the control up to the 5th day of storage. However, the level of anthocyanins in this sample gradually decreased as the storage period extended. After 10 days, the loss of anthocyanins in the fruit with essential oil was around 37%.

Quality and antioxidant activity of highbush blueberry fruit coated with starch-based and gelatine-based film enriched with cinnamon oil. 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.

An efficient copper-catalyzed C-H/N-H bond functionalization for the synthesis ¦Á-keto-N-acyl sulfoximines from aryl Me ketones and NH-sulfoximines with mol. oxygen as terminal oxidant has been developed. E.g., under an atm. of dioxygen, CuBr in DMSO catalyzed the reaction of PhCOMe and PhSMe(O)(:NH) to give 74% PhCOCON:SMePh(O).

Copper-Catalyzed Oxidative ¦Á-Ketoacylations of Sulfoximines with Aryl Methyl Ketones and Dioxygen as Terminal Oxidant. 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.

An iron-catalyzed dealkylative acylation of N-alkylsulfoximines RN=S(O)R1R2 [R = CH3, CH3(CH2)3, (CH2)9CH=CH, etc.; R1 = CH3, C6H5, 4-ClC6H4, 4-BrC6H4, 4-H3COC6H4; R2 = CH3, C6H5, c-C3H5; R1R2 = -(CH2)4-] has been developed. This process involves a Polonovski-type dealkylation of an N-alkylated sulfoximine to afford a reactive intermediate that is trapped in the presence of a suitable aldehyde R3CHO (R3 = C6H5, 2-H3CC6H4, 3-ClC6H4, etc.) or anhydride R4C(O)OC(O)R4 [R = CH3, CH3(CH2)4, C6H5CH=CH, etc.] to afford N-acylsulfoximine derivatives R1R2S(O)=NR4 and N-aroylsulfoximine derivatives R1R2S(O)=NR3 in one pot. Subsequent cleavage of the acyl or aroyl group under acidic conditions generates a synthetically valuable NH-sulfoximines R1R2S(O)=NH.

Iron-Catalyzed Acylative Dealkylation of N-Alkylsulfoximines. 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.

Varroosis is a disease caused by the mite Varroa destructor, and it is considered one of the biggest threats to honey bee populations globally. Mite control is centered on the use of synthetic acaricides, such as amitraz and flumethrine. However, high usage of these chems. is associated with a wide variety of undesirable effects on bee colonies, including the development of resistance and persistence of harmful residues of acaricides in hive products used by humans. Botanical extracts have been identified as a potentially suitable organic alternative to synthetic acaricides. Essential oils, such as clove, eucalyptus, lemongrass, and oregano, have been found to exhibit acaricidal activity against V. destructor. The main goal of this work was to assess the bioactivity of the Cymbopogon nardus essential oil from two different locations (Argentina and India), and the activity of its major component the monoterpene citronellal. According to our results, complete essential oil from India is more effective in controlling parasitosis than the isolated citronellal component. The essential oil of C. nardus from Argentina demonstrated promise for the control of varroosis, as well as exhibiting low toxicity against bees (LC50 = 11.84 ¦ÌL/mL). In addition, this essential oil may avoid the problems caused by synthetic acaricides, such as the emergence of resistance foci in Varroa and residues in hive products. Future research needs to investigate the delivery of volatile essentials oils to target mite populations.

Lethal concentrations of Cymbopogon nardus essential oils and their main component citronellal on Varroa destructor and Apis mellifera. 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.

2,3-Cl2C6H3NH2 (20 g.) added dropwise to 120 cc. ClSO3H, the mixture heated 48 hrs. at 110¡ã, cooled, poured onto ice, filtered, the residue added in small portions to liquid NH3, the NH3 evaporated, the residue dissolved twice in hot dilute NH4OH, and reprecipitated with AcOH gave 10.8 g. 6,5,4,1,3-Cl2(H2N)C6H(SO2NH2)2, m. 293-4¡ã. 2,5-Cl2C6H3NH2 (I) (10 g.) in 60 cc. ClSO3H heated 4 hrs. at 125¡ã, hydrolyzed, and treated in the usual manner with NH3 yielded 7.8 g. 5,2,4,1,3-Cl2(H2N)C6H(SO2NH2)2, needles, m. 258-9¡ã (EtOH). A similar run at 170¡ã during 0.5 hr. gave the monosulfonamide (II) of I, which refluxed 2 hrs. in ClSO3H, hydrolyzed, and treated with NH3 did not give a pure product. II (5.8 g.), 1.0 g. 5% Pd-C, 20 cc. 5N NaOH, and 100 cc. H2O hydrogenated 15 min. at 2 atm., filtered, and acidified gave 12.5 g. 4,6,2-Cl2(H2N)C6H2SO2NH2 (III), needles, m. 162-2¡ã (H2O). III refluxed 4 hrs. in ClSO3H and treated with NH3 gave a small amount of a mixture of III and the desired disulfonamide. III (5.7 g.) dehalogenated catalytically in the usual manner yielded 2.35 g. o-H2NC6H4SO2NH2, m. 153-4.5¡ã. 3,4-Cl2C6H3NH2 (10 g.) in 60 cc. ClSO3H heated 4 hrs. at 125¡ã, hydrolyzed, and treated with NH3 in the usual manner gave 5.5 g. 4,5,2-Cl2(H2N)C6H2SO2NH2, m. 175.5-6.5¡ã (aqueous Me2CO). 4,2-Cl(O2N)C6H3SO2NH2 (19 g.) in EtOH hydrogenated at low pressure over Pd-C gave 12.2 g. 4,2-Cl(H2N)C6H3SO2NH2, m. 144-6¡ã. The appropriate sulfonamide in 98% HCO2H refluxed 2 hrs., poured into H2O, and filtered gave 73-94% of the corresponding 1,2,4-benzothiadiazine 1,1-dioxide (IV); in this manner were prepared the following compounds (m.p. given): IV, 221-2¡ã (iso-PrOH); 5,6-dichloro-7-sulfamoyl derivative (V) of I, 314-15¡ã; 6,8-di-Cl derivative (VI) of I, 309-10¡ã; 6,7,-di-Cl derivative (VII) of I, 310-11¡ã (iso-PrOH); 6-Cl derivative (VIII) of I, 255-6¡ã. The appropriate sulfonamide in H2O, Me2CO, or aqueous Me2CO containing formalin refluxed 2 hrs., cooled (when Me2CO was used, diluted with H2O), and filtered gave 83-97% of the corresponding 3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxide; in this manner were prepared the 3,4-dihydro derivatives of the following compounds (m.p. given): V, 302-3¡ã; VI, 249-50¡ã; VII, 207-9¡ã; IV, 171-2¡ã (H2O or iso-PrOH); VIII, 172-3¡ã. V was slightly more potent than chlorothiazide (IX). Dihydro derivative of V was more active as a diuretic than IX, but not as active as dihydro derivative of IX.

Synthesis of potential diuretic agents. II. Dichloro derivatives of 1,2,4-benzothiadiazine 1,1-dioxide. 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