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Title:
PREPARATION METHOD OF 2-((4R, 6S)-6-BROMOMETHYL-2, 2-DIMETHYL-1, 3-DIOXANE-4-YL)ACETATE
Document Type and Number:
WIPO Patent Application WO/2016/074324
Kind Code:
A1
Abstract:
Provided is a preparation method of 2-((4R, 6S)-6-bromomethyl-2, 2-dimethyl-1, 3-dioxane-4-yl)acetate (I). Such compound is a key chiral intermediate in preparing a statins lipid-lowering drugs. The method comprises: carrying out a bromination cyclization reaction on 3-((substituted oxyformyl)oxy)-5-hexenoate (II) with a bromination reagent in an organic solvent in the presence of an inorganic base to obtain 2-((4R, 6S)-6-bromomethyl-2-oxo-1, 3-dioxane-4-yl)acetate (III), and then carrying out a ketalation reaction with a ketalation reagent in the presence of a protonic acid to obtain the 2-((4R, 6S)-6-bromomethyl-2, 2-dimethyl-1, 3-dioxane-4-yl)acetate (I). The method has readily available raw material, mild conditions, simple operation and low cost, thus facilitating industrial production.

Inventors:
CHEN FENER (CN)
XIONG FANGJUN (CN)
WU YAN (CN)
CHEN WENXUE (CN)
CHEN WEIQI (CN)
Application Number:
PCT/CN2014/095502
Publication Date:
May 19, 2016
Filing Date:
December 30, 2014
Export Citation:
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Assignee:
UNIV FUDAN (CN)
International Classes:
C07D319/06
Domestic Patent References:
WO2003053950A12003-07-03
Foreign References:
CN101735272A2010-06-16
Attorney, Agent or Firm:
SHANGHAI PATENT & TRADEMARK LAW OFFICE, LLC (CN)
上海专利商标事务所有限公司 (CN)
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