Heterocyclic Building Blocks-Benzoxazole

(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 facile protocol for direct oxidative C-N bond coupling of unactivated imidazo[1,2-a]pyridines with NH-sulfoximines was disclosed using sulfoximines as the nitrogen sources in the presence of (diacetoxy)iodobenzene (PhI(OAc)2). The reaction proceeded smoothly under air without any metal catalyst to give a series of C-3 sulfoximidoyl-functionalized imidazo[1,2-a]pyridines products regioselectively.

PhI(OAc)2-mediated oxidative C-H sulfoximination of imidazopyridines under mild 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) are substances with biol. properties that can be used to inhibit insects and fungi in storage systems. The EOs from plants of the genus Melaleuca (Myrtaceae) show insecticidal and antifungal activities. However, so far, there are no reports regarding Melaleuca rhaphiophylla (Myrtaceae) EO. Therefore, we sought to investigate the insecticidal and antifungal activities of M. rhaphiophylla EO against storage pests and fungi. The plant’s EO was extracted in a vat using the steam drag method and analyzed by gas chromatog.-mass spectrometry. The insecticidal effect against Sitophilus zeamais and Sitophilus oryzae (Coleoptera: Curculionidae) was evaluated through contact and fumigation methods in order to select the optimized exposure route. Then, the lethal concentration (LC), lethal time (LT), and mean survival time (MST) were estimated Antifungal activity against Aspergillus flavus, Aspergillus niger, Aspergillus nomius and Fusarium graminearum was tested through volatilization and direct contact. Twenty-two compounds were identified in the chem. composition of M. rhaphiophylla EO and the major compounds were ¦Á-terpinene (6.46%), 1,8-cineole (11.54%), ¦Ã-terpinene (13.2%), terpinolene (28.72%) and terpinen-4-ol (19.82%). The fumigation method of application caused the highest mortality in both insects. The values for LC50 (90.55 and 72.88 of substance L-1 of air), LT50 (0.92 and 1.23 h) and MST (92.17 and 92.67 h) were similar between species (S. zeamais and S. oryzae, resp.). The volatilization method showed low fungicidal activity (< 30% of inhibition) against all isolates. The contact method showed an inhibition greater than 90%with higher toxicity for Aspergillus. Our results showed that M. rhaphiophylla EO has potential as an alternative product to control storage pests and fungi. Insecticidal and antifungal activities of Melaleuca rhaphiophylla essential oil against insects and seed-borne pathogens in stored products. 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.

Angelica sylvestris L. var. stenoptera Ave-Lall ex Boiss. (ASS) is an endangered endemic plant to Turkey. The objective of the study was to determine antioxidant activities, total phenolics, and phytochem. properties of methanolic extracts (MEs) and essential oil (EO) from ASS for the first time with the methods of 2,2-diphenyl-1-picrylhydrazyl (DPPH¡¤) radical scavenging activities, 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS¡¤+), ferric reducing/antioxidant power (FRAP), the Folin-Ciocalteu, liquid chromatog.-tandem mass spectrometry (LC-MS/MS), and gas chromatog.-mass spectrometry (GC-MS), resp. The leaf extract of ASS was found to be the richest in phenolic content (543.91¡À6.33 GAE, ¦Ìg/mL) and showed the highest DPPH¡¤ and FRAP activities (IC50: 0.1140¡À0.0011 mg/mL, 675.62¡À15.01 ¦ÌM TEAC). EO of ASS root showed DPPH¡¤ and FRAP activities (IC50: 1.3248¡À0.0572 mg/mL, 346.67¡À12.75 ¦ÌM TEAC). 19 phenolics were detected in MEs of different parts of ASS by LC/MS/MS. In the chem. composition of ASS root EO by GC/MS, globulol (70.70 %) was found to be the major compound Our results indicate that ASS can be used a source of phytochems. and antioxidants for conservation and sustainability of endangered plants.

Phytochemical Composition and Biological Activities of Angelica sylvestris L. var. stenoptera Ave-Lall ex Boiss.: An Endangered Medicinal Plant of Northeast Turkey. 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 iron-catalyzed C-N bond formation by hetero-cross-dehydrogenative coupling (CDC) between sulfoximines and diarylmethanes is described. The reaction shows good functional group tolerance and provides N-alkylated sulfoximines in moderate to good yields.

Iron-Catalyzed Hetero-Cross-Dehydrogenative Coupling Reactions of Sulfoximines with Diarylmethanes: A New Route to N-Alkylated 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

(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 tetrabutylammonium tribromide-mediated three-component reaction of alkenes, diselenides, and sulfoximines was established herein, providing direct and metal-free access to diverse ¦Â-arylseleno sulfoximine derivatives I [R1 = Ph, 4-MeC6H4, 4-FC6H4, etc.; R2 = Ph, 4-FC6H4, 2-MeC6H4, etc.; R3 = Me, Et, cyclopropyl; R4 = Et, Ph, 4-BrC6H4, etc.]. This regioselective sulfoximido-selenization protocol proceeds efficiently under mild and ambient conditions with generally good yields. This strategy was featured by step and atom economy, practicability, a broad substrate scope, and gram-scale synthesis.

Synthesis of ¦Â-Arylseleno Sulfoximines: A Metal-Free Three-Component Reaction Mediated by Tetrabutylammonium Tribromide. 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

4-(S-Methylsulfonimidoyl)benzonitrile (BD00975057) 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 palladium-catalyzed aroylation of NH-sulfoximines for the efficient synthesis of N-aroyl sulfoximines from aryl halides and chloroform was developed. The mild reaction conditions (temperature, catalyst loading) and the use of a CO surrogate rendered this transformation a useful method for the synthesis of N-aroyl sulfoximines from available feedstock.

Palladium catalyzed aroylation of NH-sulfoximines with aryl halides using chloroform as the CO precursor. 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

(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.

Bismuth drugs have long been used against gastrointestinal diseases, especially the gastric infection of Helicobacter pylori. Cisplatin is a widely used anticancer drug that tends to accumulate at renal proximal tubules and causes severe nephrotoxicity. It was found that bismuth pretreatment reduces cisplatin-induced nephrotoxicity, but the mechanism of action remains unclear. To understand bismuth’s effect on renal tubules, we profiled the proteomic changes in human proximal tubular cells (HK-2) upon bismuth treatment. We found that bismuth induced massive glutathione biosynthesis, glutathione S-transferase activity, and vesicular transportation, which compartmentalizes bismuth to the vesicles and forms bismuth-sulfur nanoparticles. The timing of glutathione induction concurs that of bismuth-induced cisplatin toxicity mitigation in HK-2, and bismuth enhanced cisplatin sequestration to vesicles and incorporation into bismuth-sulfur nanoparticles. Finally, we found that bismuth mitigates the toxicity of general soft metal compounds but not hard metal compounds or oxidants. It suggests that instead of through oxidative stress reduction, bismuth reduces cisplatin-induced toxicity by direct sequestration.

Bismuth reduces cisplatin-induced nephrotoxicity via enhancing glutathione conjugation and vesicular transport. 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-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 copper-catalyzed N-silylation of sulfoximines was achieved in the presence of di-tert-Bu peroxide. Notably, alkyl, Ph and alkoxyl silanes were all suitable reaction partners. Mechanistic studies revealed that N-silyl acetamide serves as the intermediate.

The N-silylation 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-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.

Air- and moisture-stable N-trifluoromethylthio sulfoximines, R1R2S(O):NSCF3 (R1 = Ph, cyclopropyl, Me, CF3, R2 = Ph, 4-BrC6H4, 2-ClC6H4, etc.), have been prepared from N-H-sulfoximines via the corresponding N-Br derivatives in excellent yields. The two-step process starts with an easy-to-perform bromination at the sulfoximine nitrogen, followed by a reaction with silver trifluoromethanethiolate. A one-pot reaction sequence allows difficult to prepare products to be obtained.

N-Trifluoromethylthiolated 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.

Plant volatile organic compounds (PVOCs) have shown great potential as alternatives to synthetic insecticides or fungicides for stored grain management. Zanthoxylum schinifolium pericarp, a traditional Chinese spice, is conventionally buried in grain piles to prevent fungal spoilage of stored grains in China. However, the chem. basis and antifungal mechanism of PVOCs from Z. schinifolium pericarp by which they inhibit spoilage remain unclear. In this study, the effectiveness of PVOCs from Z. schinifolium pericarp against Aspergillus flavus growth in high-moisture wheat grains was studied under simulated storage conditions. The growth of A. flavus in the grains was inhibited in a dose-dependent manner. The chem. composition of PVOCs from Z. schinifolium pericarp was determined using gas chromatog.-mass spectrometry; linalool (50.31%) and D-limonene (20.92%) were the two main components. An antifungal experiment showed that 0.571 and 1.2 ¦ÌL/mL concentrations of linalool completely inhibited A. flavus growth upon vapor and liquid contact, resp. D-limonene showed much lower antifungal activity, indicating that linalool is responsible for the antifungal activity of PVOCs from Z. schinifolium pericarp. Linalool treatment disrupted the cell membrane of A. flavus, resulting in increased electrolyte leakage and A260nm in the culture supernatant. After 6 h of exposure to 1.2 ¦ÌL/mL linalool, metabolomic anal. revealed 90 differentially expressed metabolites in A. flavus mycelia, including 69 upregulated and 21 downregulated metabolites. It was speculated that linalool inhibited A. flavus by disrupting the permeability and integrity of cell membranes, tricarboxylic acid cycle, and ATP binding cassette transport and by inducing mitochondrial dysfunction and oxidative stress. This study shows the potential of PVOCs from Z. schinifolium pericarp as biofumigants for stored grain management and provides a new perspective on their antifungal mechanism against A. flavus growth.

Linalool, the main volatile constituent from Zanthoxylum schinifolium pericarp, prevents growth of Aspergillus flavus in post-harvest grains. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem