L. Jinping, Jiao Shu-qing, Yang Mingbo
2013
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Journal
Chinese Journal of Medicinal Chemistry
Abstract
Eberconazole nitrate is a topical,broad-spectrum imidazole derivative,effective in pitynasis dermatophytoses and candidiasis. In order to optimize the synthesis of eberconazole nitrate,a new synthetic route w as designed. The key intermediate 2,4-dichloro-10,11-dihydro-5H-dibenzo[a,d] cycloheptene-5-one( 5)w as synthesized from 3,5-dichloro benzyl bromide via Wittig reaction,hydrogenation,hydrolysis,cyclization. Then,reduction,chlorination,alkylation and salification w ere combined into one step from the intermediate 5 to eberconazole nitrate. The procedure developed has several advantages such as mild reaction conditions,short process route and easy industrial production. The overall yield of the target compound w as 26%.