Chen Yong-hao, Long Sheng-jing
2008
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Journal
Chinese Journal of Pharmaceuticals
Abstract
Antifugal drug ketoconazole was synthesized by utilization of phase-transfer catalysis from [2-bromomethyl-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl] methanol via acylation,N-alkylation with imidazole and hydrolysis,formation the active ester with methanesulfonyl chloride,and then condensation with the side chain 1-acetyl-4-(4-hydroxyphenyl)piperazine with an overall yield of about 30%.