LEE, MI YOUNGKR,이미영,LEE, KUN HEEKR,이건희,KWON, JAE WOOKKR,권재욱,SEO, MYEONG WONKR,서명원,KANG, JAE HOONKR,강재훈
申请号：
KR1020150148074
公开号：
KR1020170047686A
申请日:
2015.10.23
申请国别(地区):
KR
年份:
2017
代理人:
摘要：
The present invention relates to an improved method for preparing 2-oxo prasugrel, 5-(&alpha-cyclopropylcarbonyl-2-fluorobenzyl)-2-oxo-2,4,5,6,7,7a-hexahydrothieno[3,2,-c]pyridine (chemical formula 1), which is a major intermediate of prasugrel. More specifically, the present invention provides an improved method which is characterized by adding water as a catalyst and dividedly feeding an inorganic basic composition when 2-oxo prasugrel is synthesized through a condensation reaction between &alpha-cyclopropylcarbonyl-2-fluorobenzylbromide represented by chemical formula 2 and 2-oxo-2,4,5,6,7,7a-hexahydrothieno[3,2,-c]pyridine hydrochloride represented by chemical formula 3.COPYRIGHT KIPO 2017본 발명은 하기 프라수그렐의 주요 중간체인 2-옥소 프라수그렐, 5-(α-시클로프로필카르보닐-2-플루오로벤질)-2-옥소-2,4,5,6,7,7a-헥사히드로티에노[3,2,-c]피리딘(화학식 1)의 개선된 제조방법에 관한 것이다. 보다 상세하게는 화학식 2로 표시되는 α-시클로프로필카르보닐-2-플루오로벤질브로마이드와 화학식 3으로 표시되는 2-옥소-2,4,5,6,7,7a-헥사히드로티에노[3,2-c]피리딘 염산염의 축합반응을 통하여 2-옥소 프라수그렐을 합성함에 있어서 물을 촉매로 추가하고, 무기 염기성 화합물을 분할 투입하는 것을 특징으로 하는 개선된 제조 방법을 제공하는 것이다. 화학식 1화학식2화학식 3
