Miao Zhen-yuan
2006
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Journal
Chinese Journal of Medicinal Chemistry
Abstract
Aim To improve the synthetic process of 4-[4-(5oxo-1,5-dihydro-triazoyl-4-yl)phenyl] piperazine-1-carboxylic t-butyl ester,which is used as the key intermediate of triazole antifungal agents.Methods The product was synthesized from 1-(4-nitrophenyl)piperazine by Boc protection,reduction of nitro group,acylation,hydrazinolysis and cyclization.Results and conclusion The new synthetic process has several advantages such as facile reaction condition,convenient operation and purification without chromatography.The overall yield is improved from 39.10% to 71.94%.