170863-69-1

Upstream product

• 51336-94-8 2-chloro-1-(2,4-dichlorophenyl)ethanone 
• 672324-84-4 4-(thiazol-2-yl)benzonitrile 
• 1026500-07-1 4-{5-[2-Chloro-1-(2,4-difluoro-phenyl)-1-hydroxy-ethyl]-thiazol-2-yl}-benzonitrile 
• 170863-68-0 1-(2,4-difluorophenyl)-1-[4-(4-cyanophenyl)thiazol-5-yl]-2-(1H-1,2,4-triazol-1-yl)ethanol 

Relevant academic research and scientific papers

Azole antifungal agents, processes for the preparation thereof, and intermediates

A compound represented by the general formula: wherein R1 and R2 denote a halogen atom or hydrogen atoms; R3 means a hydrogen atoms or lower alkyl group; r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic rings, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for -S-, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmacetical composition suitable for use as an antifungal agent.

Synthesis and antifungal activity of novel thiazole-containing triazole antifungals

A new series of thiazole-containing triazole antifungals was synthesized and evaluated for antifungal activity against a variety of clinically isolated pathogenic fungi in vitro and against systemic candidosis in vivo. Among these compounds, (±)-1-(2,4-difluorophenyl)-1-[4-(2,4- difluorophenyl)thiazol-2-yl]-2-(1H-1,2,4-triazol-1-yl)ethanol (ER24161) showed the most potent and well-balanced in vitro activities and excellent in vivo efficacy. We also achieved an enantioselective synthesis of the more potent enantiomer of ER-24161.