68070-62-2

Upstream product

• 95-16-9 1,3-Benzothiazole 
• 103-71-9 phenyl isocyanate 
• 62-53-3 aniline 
• 137-07-5 2-amino-benzenethiol 
• 32137-76-1 benzothiazole-2-carboxylic acid ethyl ester 
• 3622-04-6 2-carboxybenzothiazole 
• 127427-45-6 2-bromo-2,2-difluoro-N-phenyl-acetamide 
• 6890-75-1 Phenylaminothioxoacetic Acid 
• 56934-77-1 2-thioxo-2-phenylaminoacetic acid ethyl ester 
• 6244-74-2 N,N'-diphenyldithiooxamide 
• 1457-85-8 Ethyl oxanilate 
• 73042-64-5 2H-1,4-benzothiazine-2,3⁽⁴⁾-dione 
• 78121-70-7 N,N'-diphenylthiooxamide 

Relevant academic research and scientific papers

S8-Catalyzed triple cleavage of bromodifluoro compounds for the assembly of N-containing heterocycles

An unprecedented S8-catalyzed selective triple-cleavage of bromodifluoroacetamides is disclosed for the first time. Valuable 2-amido substituted benzimidazoles, benzoxazoles and benzothiazoles were obtained in good to excellent yields in a casc

Benzo[d]thiazole-2-carbanilides as new anti-TB chemotypes: Design, synthesis, biological evaluation, and structure-activity relationship

Tuberculosis is the second leading cause of deaths worldwide. The inadequacy of existing drugs to treat TB due to developed resistance and TB-HIV synergism urges for new anti-TB drugs. Seventy-two benzo[d]thiazole-2-carbanilides have been synthesized through CDI-mediated direct coupling of benzo[d]thiazole-2-carboxylic acids with aromatic amines using a three step methodology which includes a green protocol for synthesis of ethyl benzo[d]thiazole-2-carboxylates, precursor of the desired carboxylic acids. The compounds were evaluated in vitro for anti-tubercular activity against M. tuberculosis H37Rv (ATCC27294 strain). Thirty-two compounds exhibiting MIC values in the range of 0.78–6.25 μg/mL (1.9–23 μM) were subjected to cell viability test against RAW 264.7 cell lines and thirty compounds were found to be non-toxic (50% inhibition). The most active compounds with MIC of 0.78 μg/mL (e.g., 4i, 4n, 4s, 4w, 6f, 6h, 6u, 7e, 7h, 7p, 7r and 7w) exhibit therapeutic index of 64. The structure activity relationship of the N-arylbenzo[d]thiazole-2-carboxamides has been established for anti-mycobacterial activity. Molecular docking suggests that the compounds 7w, 4i and 4n bind to the catalytic site of the enzyme ATP Phosphoribosyltransferase (HisG) and might be attributed to their anti-TB potential. These can serve as a new starting point for the development of anti-TB agents with therapeutic potential.

Azole-N-acetonitriles as carbonyl synthons: A one-pot preparation of heteroaryl amides from halides

Azole-N-acetonitrile derivatives were utilized as synthons for an ambident carbonyl moiety via a strategy relying upon sequential base-mediated S NAr substitution of a 2-halo heterocycle, in situ oxidation, and amine displacement. This strategy allows prompt and efficient synthesis of N-containing heteroaryl amides directly from the corresponding halides via a one-pot process.