专利详情

专利名称	PROCESS FOR SYNTHESIS OF EZETIMIBE AND INTERMEDIATES USED IN SAID PROCESS
申请号	EP20130819243	专利类型	EP
公开（公告）号	EP2876102(B1)	公开（授权）日	2016.12.07
申请（专利权）人	中国科学院上海有机化学研究所	发明（设计）人	DING, Kuiling;WANG, Xiaoming;WANG, Zheng
主分类号	C07C67/34	IPC主分类号	C07C67/34;C07C69/73;C07F9/50;C07F15/00
专利有效期	PROCESS FOR SYNTHESIS OF EZETIMIBE AND INTERMEDIATES USED IN SAID PROCESS 至PROCESS FOR SYNTHESIS OF EZETIMIBE AND INTERMEDIATES USED IN SAID PROCESS	法律状态
说明书摘要	A process for the production of ezetimibe and intermediates used in said process are disclosed. A kind of Morita-Baylis-Hillman adduct can be altered to chiral carboxylic acid derivatives of ?-arylamino ±-methylene with high activity and selectivity by means of ally lamination reaction, and the above carboxylic acid derivatives of ?-arylamino ±-methylene can be altered to the chiral intermediates of ezetimibe by means of simple conversion and further synthesized into the chiral drug ezetimibe. The synthesis route introduces chirality through the use of a chiral catalysis method, thereby avoiding the use of the chiral auxiliary oxazolidinone; and the route is economical and eco-friendly.