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Title:
EFINACONAZOLE PREPARATION METHOD AND CRYSTAL FORM M OF EFINACONAZOLE
Document Type and Number:
WIPO Patent Application WO/2018/036416
Kind Code:
A1
Abstract:
An Efinaconazole preparation method, a crystal form M of Efinaconazole, and a crystal form M preparation method. The Efinaconazole preparation method comprises: enabling 4-methylenepiperidine hydrochloride or an acid addition salt thereof and (2R,3S)-2-(2,4-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazole-1-group)methyl] ethylene oxide to undergo a reaction in a solution in the presence of at least one of reagents selected from metal alkoxide M(OR1)n, metal halide MYn or metal oxide MnO, so as generate Efinaconazole. The reaction formula is as follows. In the preparation method, the reaction is complete, the reaction condition is moderate, the yield rate is high, the selectivity is good, and the Efinaconazole having the purity higher than 99% can be obtained by means of simple processing.

Inventors:
ZHANG JIAN (CN)
TAN HONGJIAN (CN)
Application Number:
PCT/CN2017/097803
Publication Date:
March 01, 2018
Filing Date:
August 17, 2017
Export Citation:
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Assignee:
TOPHARMAN SHANDONG CO LTD (CN)
International Classes:
C07D401/06
Domestic Patent References:
WO2016181306A12016-11-17
WO2016193917A12016-12-08
Foreign References:
US20170129874A12017-05-11
CN103080100A2013-05-01
Attorney, Agent or Firm:
KINGSOUND & PARTNERS (CN)
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