专利号:US-10626102-B2 优先权日:2015-12-30 标题 :Process for the synthesis of efinaconazol 发明人:VERONESE MARTINO; BETTONI PIERGIORGIO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of efinaconazole (I), starting from 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole and 4-methylenepiperidine, as free base or hydrochloride, in an organic solvent, under anhydrous conditions and in the presence of neutralising agents and reaction-promoting metal species. (1) The process is particularly advantageous because it gives rise to efinaconazole in high yields and purity, and uses little more than the stoichiometric amount of 4-methylenepiperidine, a rather expensive commercially available reagent.
专利号:EP-3091007-A1 优先权日:2015-05-08 标 题 :Process for the preparation of piperidine compounds 发明人:ATTOLINO EMANUELE; RIZZO ELISABETH; ROSSI DAVIDE 权利人:DIPHARMA FRANCIS SRL 摘要:The present invention relates to a process for the preparation of intermediates useful in the synthesis of efinaconazole and their use in the synthesis of efinaconazole.
专利号:CN-116589447-A 优先权日:2023-04-28 标 题 :A chemical-enzyme process synthesis method of efluconazole