Category: 20582-55-2

Luo, Kai; Chen, Yao-Zhong; Chen, Li-Xian; Wu, Lei published the artcile< Autoxidative C(sp2)-P Formation: Direct Phosphorylation of Heteroarenes under Oxygen, Metal-Free, and Solvent-Free Conditions>, Synthetic Route of 20582-55-2, the main research area is phosphorylation heteroarene arylphosphine oxide; heteroaryl phosphine oxide preparation.

The authors reveal here a direct autoxidative phosphorylation of heteroarenes induced by O under metal-free and solvent-free conditions. This new methodol. provides an economical, operationally simple, and environmentally friendly approach toward (Het)C(sp2)-P formation with medium to excellent yields. Heteroarenes including thiazole and quinoxaline derivatives are applicable under standard conditions, which is testified via a radical mechanism.

Journal of Organic Chemistry published new progress about Aromatic hydrocarbons Role: RCT (Reactant), RACT (Reactant or Reagent) (heteroarenes). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Synthetic Route of 20582-55-2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Wang, Xinmou; Chen, Yuming; Song, Hongjian; Liu, Yuxiu; Wang, Qingmin published the artcile< Construction of 2-(2-Arylphenyl)azoles via Cobalt-Catalyzed C-H/C-H Cross-Coupling Reactions and Evaluation of Their Antifungal Activity>, COA of Formula: C7H9NO2S, the main research area is biaryl azole cobalt catalyst agrochem fungicide; azole biphenyl amide cross coupling reaction.

Although compounds with a 2-(2-arylphenyl) benzoxazole motif are biol. important, there are only a few methods for synthesizing them. Herein, authors report an efficient method for synthesis of such compounds by means of cobalt-catalyzed C-H/C-H cross-coupling reactions. This method has a broad substrate scope and good tolerance for sensitive functional groups. In addition, authors demonstrate that introducing a heteroarene moiety to biphenyl compounds enhanced their antifungal activity.

Organic Letters published new progress about Agrochemical fungicides. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, COA of Formula: C7H9NO2S.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Hagiya, Kazutake; Mitsui, Sunao; Taguchi, Hiroaki published the artcile< A facile and selective synthetic method for the preparation of aromatic dialdehydes from diesters via the amine-modified SMEAH reduction system>, Application In Synthesis of 20582-55-2, the main research area is facile synthetic preparation aromatic dialdehyde diester amine SMEAH reduction.

A new reduction system employing N-methylpiperazine-modified sodium bis(2-methoxyethoxy)aluminum hydride (NMP-SMEAH) for the conversion of aromatic diesters to dialdehydes is described. The method is plain and efficient, and can be carried out under mild and operationally simple conditions applicable for large scale productions.

Synthesis published new progress about Dialdehydes Role: SPN (Synthetic Preparation), PREP (Preparation). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Application In Synthesis of 20582-55-2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Wu, Yue; Guo, Peng; Chen, Long; Duan, Weijie; Yang, Zengzhuan; Wang, Tao; Chen, Ting; Xiong, Fei published the artcile< Iron-catalyzed tandem oxidative coupling and acetal hydrolysis reaction to prepare formylated benzothiazoles and isoquinolines>, COA of Formula: C7H9NO2S, the main research area is azole dioxolone iron tandem Minisci type oxidative coupling hydrolysis; carbonyl azole preparation green chem; isoquinoline dioxolone iron tandem Minisci type oxidative coupling hydrolysis; formylisoquinoline preparation green chem.

The direct formylation of benzothiazoles and isoquinolines was reported. The reaction features a novel iron-catalyzed Minisci-type oxidative coupling process using com. available 1,3-dioxolane as a formylated reagent followed by acetal hydrolysis without a separation process. The reaction was performed under exceedingly mild reaction conditions and exhibited broad functional group tolerance.

Chemical Communications (Cambridge, United Kingdom) published new progress about Alkyl aryl ketones Role: SPN (Synthetic Preparation), PREP (Preparation). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, COA of Formula: C7H9NO2S.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Farmer, Luc J.; Bemis, Guy; Britt, Shawn D.; Cochran, John; Connors, Martin; Harrington, Edmund M.; Hoock, Thomas; Markland, William; Nanthakumar, Suganthini; Taslimi, Paul; Ter Haar, Ernst; Wang, Jian; Zhaveri, Darshana; Salituro, Francesco G. published the artcile< Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK)>, Electric Literature of 20582-55-2, the main research area is pyrimidine phenylamino thiazolyl derivative preparation tyrosine kinase inhibition SAR; phenylamino pyrimidine thiazole derivative preparation mast cell degranulation inhibition.

A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead, I, were prepared and evaluated for biol. activity. Lead optimization provided compounds with nanomolar Ki’s against SYK and potent inhibition in mast cell degranulation assays.

Bioorganic & Medicinal Chemistry Letters published new progress about Animal gene, c-src Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Electric Literature of 20582-55-2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Bi, Huihua; Zhou, Yu; Jiang, Wei; Liu, Jie published the artcile< Electrophotocatalytic C-H Hydroxyalkylation of Heteroaromatics with Aldehydes>, Synthetic Route of 20582-55-2, the main research area is heteroarene electrochem photochem Minisci hydroxyalkylation aldehyde; alc heteroaryl preparation.

A radical hydroxyalkylation of N-heteroaromatics with aldehydes is reported. The constructive merging of photochem. and electrochem. is the key for the success of this atom-economical Minisci method. This protocol highlights the utility of electrophotocatalysis to promote a practical and general synthesis of secondary alcs. in good yields from readily available N-heteroaromatics and aldehydes under mild reaction conditions.

Advanced Synthesis & Catalysis published new progress about Aldehydes Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Synthetic Route of 20582-55-2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Fu, Xiao-Pu; Xuan, Qing-Qing; Liu, Li; Wang, Dong; Chen, Yong-Jun; Li, Chao-Jun published the artcile< Dual C-H activations of electron-deficient heteroarenes: palladium-catalyzed oxidative cross coupling of thiazoles with azine N-oxides>, Quality Control of 20582-55-2, the main research area is palladium catalyst oxidative cross coupling thiazole azine oxide; thiazolylpyridine oxide preparation.

The palladium-catalyzed, copper-promoted cross-dehydrogenative-coupling (CDC) of electron-deficient thiazoles with azine N-oxides through dual C-H activations was developed. It was found that copper(II) pivalate was an efficient dual-function reagent for the oxidative cross-coupling reactions, playing the roles of both an oxidant and a C-H bond activation promoter. E.g., in presence of Pd(OAc)2 and copper(II) pivalate, oxidative coupling of pyridine N-oxide and 6-methylbenzothiazole gave 70% 2-thiazolylpyridine derivative (I). This methodol. provides a simple way to construct the 2-thiazolylpyridine moiety.

Tetrahedron published new progress about Isotope effect. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Quality Control of 20582-55-2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Curreli, Francesca; Kwon, Young Do; Zhang, Hongtao; Scacalossi, Daniel; Belov, Dmitry S.; Tikhonov, Artur A.; Andreev, Ivan A.; Altieri, Andrea; Kurkin, Alexander V.; Kwong, Peter D.; Debnath, Asim K. published the artcile< Structure-Based Design of a Small Molecule CD4-Antagonist with Broad Spectrum Anti-HIV-1 Activity>, HPLC of Formula: 20582-55-2, the main research area is antiviral HIV AIDS.

Earlier the authors reported the discovery and design of NBD-556 and their analogs which demonstrated their potential as HIV-1 entry inhibitors. However, progress in developing these inhibitors has been stymied by their CD4-agonist properties, an unfavorable trait for use as drug. Here, the authors demonstrate the successful conversion of a full CD4-agonist (NBD-556) through a partial CD4-agonist (NBD-09027), to a full CD4-antagonist I (NBD-11021) by structure-based modification of the critical oxalamide mid-region, previously thought to be intolerant of modification. I showed unprecedented neutralization breath for this class of inhibitors, with pan-neutralization against a panel of 56 Env-pseudotyped HIV-1 representing diverse subtypes of clin. isolates (IC50 as low as 270 nM). The cocrystal structure of NBD-11021 complexed to a monomeric HIV-1 gp120 core revealed its detail binding characteristics. The study is expected to provide a framework for further development of NBD series as HIV-1 entry inhibitors for clin. application against AIDS.

Journal of Medicinal Chemistry published new progress about AIDS (disease). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, HPLC of Formula: 20582-55-2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Komiyama, Masato; Tsuchiya, Hideyoshi; Teramoto, Mitsuru; Yajima, Naoki; Kurokawa, Masayuki; Minamizono, Kunio; Tsuchiya, Naoki; Kato, Yoshiaki; Sato, Yoshinori; Dohi, Masahiko published the artcile< Process Development of Febuxostat Using Palladium- and Copper-Catalyzed C-H Arylation>, Electric Literature of 20582-55-2, the main research area is Febuxostat process synthesis palladium copper catalyzed arylation thiazole bromoarene.

There is significant interest in the development of process routes for active pharmaceutical ingredients using C-H arylation methodol. An efficient and practical synthetic route for febuxostat, which is the first non-purine-type xanthine oxidase inhibitor, was established via palladium- and copper-catalyzed C-H arylation of thiazole with aryl bromide. The catalyst loading was reduced to 0.1 mol % for the intermol. C-H arylation, and a three-step synthesis produced febuxostat in 89% overall yield with excellent selectivity.

Organic Process Research & Development published new progress about Arylation. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Electric Literature of 20582-55-2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Abdel-Lateef, Mahmoud F. A.; Stec, Maria; Eckstein, Zygmunt published the artcile< Systemic and chemotherapeutic fungicidal activity-chemical structure relation of some 4-methyl-5-thiazolecarboxylic acid derivatives. Laboratory screening tests>, Formula: C7H9NO2S, the main research area is methylthiazolecarboxylate derivative fungicide; structure fungicide activity thiazolecarboxylate derivative.

Of 137 synthetic 4-methyl-5-thiazolecarboxylates (I, X = H, halo, Me, SH, alkoxy, aryloxy, alkylthio, arylthio, aryloxyalkyl heterocyclic radical, etc. R = HO, alkoxy, substituted amine, etc) 108 were previously undescribed. I compounds were screened with Alternaia tenuis, Phytophthora infestans, Rhizoctonia, solani, Tilletia caries, and Venturia inaequalis for chem. structure-activity relations. The m.p., yield, and fungicidal activities of I compounds are tabulated, and their structure-activity relations are discussed.

Acta Phytopathologica Academiae Scientiarum Hungaricae published new progress about Fungicides. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Formula: C7H9NO2S.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica