Efficient one-step synthesis of a key intermediate for the synthesis of azole antifungals using the Mitsunobu protocol
A simple and single-step process for coupling (2R,1S)-1-[2-(2,4- difluorophenyl)-2-oxiranyl]ethanol and various 1,2,4-triazolones utilizing the Mitsunobu protocol is described. The product so formed is a key intermediate in the synthesis of azole antifung
Sattigeri, Jitendra A.,Arora, Jasbir S.,Verma, Ashwani K.,Malhotra, Sanjay,Salman, Mohammad
An azole compound represented by the formula (I): STR1 wherein Ar is a substituted phenyl group; R1 and R2 independently are a hydrogen atom or a lower alkyl group, or R1 and R2 may combine together to form a lower alkylene group; R3 is a group bonded through a carbon atom; R4 is a hydrogen atom or an acyl group; X is a nitrogen atom or a methine group; and n Y and Z independently are a nitrogen atom or a methine group which may optionally be substituted with a lower alkyl group, or a salt thereof, which is useful for prevention and therapy of fungal infections of mammals as antifungal agent.
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(2008/06/13)
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