公开(公告)号：US20180339974A1

公开(公告)日：2018-11-29

申请号：US15871049

申请日：2018-01-14

Applicant: FUDAN UNIVERSITY

Inventor： Fener CHEN ,  Guanxin HUANG ,  Ge MENG ,  Minjie LIU ,  Yan WU ,  Dang CHENG ,  Zedu HUANG ,  Haihui PENG ,  Fangjun XIONG

IPC: C07D319/06 ,  C07B41/12 ,  C07B47/00

CPC classification number: C07D319/06 ,  C07B41/12 ,  C07B47/00

Abstract: The present disclosure belongs to the technical field of organic synthesis and particularly relates to a preparation method for 2-((4R,6S)-6-bromomethyl-2-oxo-1,3-dioxane-4-yl)acetate. The 2-((4R,6S)-6-bromomethyl-2-oxo-1,3-dioxane-4-yl)acetate is a key chiral intermediate for preparation of statin antilipemic agents. In the present disclosure, the 2-((4R,6S)-6-bromomethyl-2-oxo-1,3-dioxane-4-yl)acetate is obtained by bromination and cyclization of 3-((substituted oxycarbonyl)oxy)-5-hexenoate as raw material with hypochlorite and bromide in an organic solvent in the presence of CO2. The method of the present disclosure has the advantages of readily available raw material, mild reaction conditions, easy operation, low cost, excellent atomic economy and less by-products, and is applicable to industrial production.