Category: benzoxazole

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 copper-catalyzed cross-dehydrogenative C-H/N-H coupling has been devised to access a series of N-arylated sulfoximines, e,g., I, in high yield from 8-aminoquinoline-derived benzamides and sulfoximines. The reaction is scalable, and mechanistic studies favor the involvement of an organometallic pathway, where C-H bond cleavage is presumed to be the kinetically relevant step. The utility of sulfoximine-coupled benzamides was displayed through the nickel-catalyzed acceptorless dehydrogenative olefination of benzyl alcs.

Copper-Catalyzed 8-Aminoquinoline-Directed Oxidative C-H/N-H Coupling for N-Arylation of 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.

American ginseng (Panax quinquefolius L.) is protected by Geog. Indications as harvested roots have different regional characteristics. The aim of this study was to distinguish 95 American ginseng samples from four origins (including America, Canada, Shandong province and the Northeast provinces in China), and to further discriminate samples harvested within the protected designation of origin (PDO) from those harvested in non-PDO regions. Two metabolomic methods were used to acquire qual. data on the metabolites of American ginseng samples from different origins, namely high-performance liquid chromatog. (HPLC) and headspace-gas chromatog.-mass spectrometry (HS-GC-MS). There were significant differences in numerous metabolites, including volatile compounds and ginsenosides. American ginsengs from four different regions were discriminated based on 25 volatile compounds and 8 ginsenosides using linear discriminant anal. (LDA), which had a 96.8% accuracy and a 74.7% cross validation rate, and random forest (RF) modeling, which reached 100% accuracy using the training set and 92.9% accuracy using the testing set. The same 33 analytes combined with LDA and RF were compared for discrimination of PDO and non-PDO samples. The 100% accuracy was again obtained using the RF model, but only when using data from both HS-GC-MS and HPLC. The result showed that chem. composition combined with chemometric is effectively and accurately to study the origins of American ginseng.

Geographical origin of American ginseng (Panax quinquefolius L.) based on chemical composition combined with chemometric. 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. 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.

Dexamethasone acts as an immunosuppressive drug and has been used recently in the management of specific coronavirus disease 2019 (COVID-19) cases; however, various adverse effects could limit its use. In this work, we studied the mitigation effects of black pepper oil (BP oil) on glycemic parameters, dyslipidemia, oxidative and nitrosative stress and pancreatic fibrosis in dexamethasone-treated rats. Animals were divided into five groups that were treated with vehicle, dexamethasone (10 mg/kg, SC) or black pepper oil (BP oil, 0.5 mL, or 1 mL/kg) or metformin (50 mg/kg) plus dexamethasone for 4 consecutive days. Serum insulin, blood glucose, total cholesterol, triglycerides, and Homeostatic Model Assessment for Insulin Resistance (HOMA-IR) were higher in the dexamethasone group vs the control group and decreased in BP oil and metformin groups relative to the dexamethasone group. Pancreatic nitric oxide, inducible nitric oxide synthase and malondialdehyde levels were increased in the dexamethasone group vs the control group and decreased in BP oil and metformin groups relative to the dexamethasone group. Pancreatic endothelial nitric oxide synthase and reduced glutathione were declined in the dexamethasone group vs the control group. They were increased in BP oil and metformin groups relative to the dexamethasone group. Moreover, the pancreatic islets diameter and collagen deposition were assessed and found to be higher in the dexamethasone group vs the control group. BP oil and metformin groups showed to regress this effect. In conclusion, BP oil may alleviate hyperglycemia, hyperinsulinemia, insulin resistance, dyslipidemia and pancreatic structural derangements and fibrosis by suppressing oxidative stress, increasing endogenous antioxidant levels, modulating nitric oxide signaling, preventing pancreatic stellate cells transition and collagen deposition.

Black pepper oil (Piper nigrum L.) mitigates dexamethasone induced pancreatic damage via modulation of oxidative and nitrosative stress. 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.

The persulfate-meditated oxidative C-N bond coupling of the C-H bond of quinoxalinones and the N-H bond of NH-sulfoximines is reported. The reaction proceeds smoothly under transition metal-free conditions and provides good to excellent yields of sulfoximidoyl-functionalized quinoxalinone products under mild conditions. The optimized conditions were found to be suitable for a range of sulfoximine and quinoxalinone substrates. This reaction offers a new and convenient strategy to directly install the sulfoximine moiety into the C3 position of quinoxalinone.

Persulfate-promoted oxidative C-N bond coupling of quinoxalinones and 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-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.

Herein, the direct N-acylation of sulfoximines with carboxylic acids promoted by a heterocyclic catalyst featuring the B3NO2 ring system have been described. The protocol used was found to be operationally simple and to tolerate a wide range of functional groups, furnishing the N-acylated sulfoximines in good yield. The multiboron catalyst tamed previously intractable nitrogen nucleophiles, allowing for the short synthesis of a factor Xa inhibitor by catalyzing two consecutive nitrogen acylations in the same pot.

Direct N-acylation of sulfoximines with carboxylic acids catalyzed by the B3NO2 heterocycle. 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.

Treating sulfoxamines PhS(O)(:NH)C6H4R-4 (R = H, Cl, NO2, Me, OMe) with Me3CONO gave reductive deimination products PhS(O)C6H4R-4 in 97-100% yields in 10-20 min. Similar treatment of MeS(O)(:NH)R1 (R1 = Ph, Me, 4-MeOC6H4) gave 96-100% MeS(O)R1 in 10-15 min. Optically active PhS(O)(:NH)Me was deiminated with no racemization. Sulfonediimines PhS(:NH)(:NSO2C6H4Me-4)R2 (R2 = Ph, C6H4R3, Me; R3 = Cl, NO2, Me, OMe) gave 99-100% PhS(:NSO2C6H4Me-4)R2 in 10-30 min on treatment with Me3CONO.

A facile conversion of sulfoximines and sulfonediimines to sulfoxides and sulfilimines with tert-butyl nitrite. 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

(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.

A novel strategy for the N-arylation of NH-sulfoximines has been developed by merging nickel catalysis and electrochem. (in an undivided cell), thereby providing a practical method for the construction of sulfoximine derivatives Paired electrolysis is employed in this protocol, so a sacrificial anode is not required. Owing to the mild reaction conditions, excellent functional group tolerance and yield are achieved. A preliminary mechanistic study indicates that the anodic oxidation of a NiII species is crucial to promote the reductive elimination of a C-N bond from the resulting NiIII species at room temperature

Nickel-Catalyzed N-Arylation of NH-Sulfoximines with Aryl Halides via Paired Electrolysis. 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.

Evidence obtained previously from in vivo experiments indicated that there are some possible relations between the diuretic actions and the physiol. dispositions of several sulfonamide diuretics. In the present investigation, tubular transport of these compounds was studied in slices of the rat kidney by a modification of the method developed by Cross and Taggart for PAH (p-aminohippuric acid) (CA 44, 6037h). Chem. determinations of these compounds were carried out by a modification of Baer, et al. (loc. cit) and S/M ratios (ratios of concentrations of drug in slice vs. medium after incubating at 25¡ã for 2 hrs.) were calculated Both HCT (hydrochlorothiazide) and PAH accumulated to a considerable degree in the renal slices. The S/M ratios of these compounds were 9.3 and 7.2, resp. However, when the incubation was carried out at 37¡ã, the S/M ratios of both drugs decreased appreciably in spite of an increase of QO2. Variations from an optimal pH of 7.8 to 8.0 towards either the acid or alk. side produced a decrease of S/M values for both drugs. Anaerobic conditions inhibited, while addition of acetate stimulated, the accumulation of HCT in the slices. Dinitrophenol (2.5 ¡Á 10-5M) or cyanide (50-100 ¡Á 10-5M) decreased the S/M values of PAH, CT (chlorothiazide), and HCT considerably. Diodrast or penicillin G, when added in concentrations 15 times as high as that of the substrate, also decreased the S/M value of HCT, without affecting the QO2 of the slices. These results suggest that HCT and its analogs may share a common renal transport mechanism with PAH, penicillin G, and Diodrast. In addition, the S/M values of 8 sulfonamide diuretics (including CT and HCT) were compared. It was found that those compounds such as HCT-55 (5-chlorohydrochlorothiazide), HCT, and HFT (hydroflumethiazide) which showed relatively high diuretic activities also exhibited higher S/M values. On the contrary, inactive compounds or compounds with low diuretic activities, such as HCT-18 (3-[3,4-dimethoxy-2-ethoxycarbonylphenyl]hydrochlorothiazide), CT, and DSA (5-chloro-2,4-disulfamylaniline) had lower S/M values. These results would be in favor of the concept that these sulfonamide derivatives exert their diuretic actions in the process of being transported by the renal tubular epithelium. CT-S (benzthiazide) accumulated in the liver slices of the rat to the same extent as in the renal slices, while HCT accumulated preferentially in the kidney slices.

Oral diuretics. IV. The uptake of some sulfonamide diuretics by rat renal slices. 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.

A mild and facile Cp*Rh(III)-catalyzed C-H activation and intramol. cascade annulation protocol has been proposed for the furnishing of highly fused isochromeno-1,2-benzothiazines I (R1 = H, 2-Me, 2-F, 4-Br, 3-OMe, (CH2)4, etc.; R2 = Me, Et, Ph, Bn, etc.; R3 = H, 10-Me,10-OMe, 11-Cl, 11-F, etc.) scaffolds using S-phenylsulfoximides R4C6H4S(O)(=NH)(R2) and 4-diazoisochroman-3-imine II (R5 = H, 7-Me, 6-OMe, 7-OMe, 6-Cl, etc.) as substrates under room temperature This method features diverse substituents and functional groups tolerance and relatively mild reaction conditions with moderate to excellent yields. Addnl., retentive configuration of sulfoximides in the conversion has been verified.

Sulfoximines-assisted Rh(III)-catalyzed C-H activation and intramolecular annulation for the synthesis of fused isochromeno-1,2-benzothiazines scaffolds under room temperature. 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-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-Vinylsulfoximines have been prepared, usually in ¡Ý90% yield, by copper-promoted coupling reactions starting from NH-sulfoximines and vinyl bromides.

A general copper-promoted coupling of sulfoximines with vinyl bromides. 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