SONG, SEOG BEOM,송석범,MOON, JEONG JU,문정주,HONG, HYE SUK,홍혜숙,PARK, MI KYUNG,박미경,CHO, IL HWAN,조일환,KWEON, JAE HONG,권재홍
申请号：
KR1020100101006
公开号：
KR1020120039344A
申请日:
2010.10.15
申请国别(地区):
KR
年份:
2012
代理人:
摘要：
PURPOSE: A manufacturing method of endoxifen is provided to lower manufacturing cost and obtain high purity edoxifen with high yield.CONSTITUTION: A manufacturing method of Z-form edoxifen which is represented by chemical formula 1 comprises the following steps: a first step of protecting one -OH in 4,4- hydroxybenzophenone using a protective group a 2nd step of coupling the outcome of the first step with propiophenone a 3rd step of O-alkylating hydroxyl group in the outcome of the 2nd step a 4th step of unprotecting the protective group which is attached to the hydroxyl group a 5th step of unprotecting a protective group of alkyl moiety which is combined by the O-alkylation and a 6th step of fractional crystallizing the outcome of the 5th step using an organic solvent.COPYRIGHT KIPO 2012본 발명은 4,4-히드록시벤조페논을 출발물질로 사용하여 프로피오페논과 커플링시켜서 엔독시펜을 제조하는 방법에 관한 것으로, 종래의 엔독시펜 제조방법에 비해 높은 수율로 E/Z 형태의 엔독시펜 혼합물을 수득하고, 혼합물 중 약효를 나타내는 Z form을 99% 이상의 순도로 제공할 수 있다.
