… Antifungal Activity of N-((1R, 2R)-2-(2, 4-Difluorophenyl)-2-hydroxy-1-methyl-3-(1H-1, 2, 4-triazol-1-yl) propyl)-N'-(4-substituted phenyl)-3 (2H, 4H)-1, 2, 4-triazolones …

…, Y MATSUSHITA, R HAYASHI, K OKONOGI…

Index: Tasaka; Teranishi; Matsushita; Tamura; Hayashi; Okonogi; Itoh Chemical and Pharmaceutical Bulletin, 1994 , vol. 42, # 1 p. 85 - 94

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Citation Number: 42

Abstract

A new series of optically active antifungal azoles, N-[(1R, 2R)-2-(2, 4-difluorophenyl)-2- hydroxy-1-methyl-3-(1H-1, 2, 4-triazol-1-yl) propyl]-N'-(4-substituted phenyl)-3 (2H, 4H)-1, 2, 4-triazolones (1, 2) and 5 (1H, 4H)-tetrazolones (3), were prepared from the triflate derivative of (1S)-1-[(2R)-2-(2, 4-difluorophenyl)-2-oxiranyl] ethanol (13) by an SN2 displacement reaction with the anion of an azolone (17-19) and subsequent ring-opening reaction with ...