HONG, YOU HWA,홍유화,LEE, YONG ARM,이용암,SHIN, HYE JUNG,신혜정
申请号:
KR1020110025370
公开号:
KR1020120107702A
申请日:
2011.03.22
申请国别(地区):
KR
年份:
2012
代理人:
摘要:
PURPOSE: A method for preparing 9-hydroxy-3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido&lsqb1,2-A&rsqbpyrimidine-4-one is provided to simply isolate a compound by column chromatography without purification.CONSTITUTION: A method for preparing a compound of chemical formula 2 comprises a step of reacting alkyl sulfonyl chloride or arylsulfonyl chloride with a compound of chemical formula 1. The aryl sulfonyl chloride is benzene sulfonyl chloride or p-toluene sulfonyl chloride. The reaction is performed under the presence of an organic base of tri-C1~C3 alkyl-amine, pyridine, or N-methyl morpholine. The reaction is also performed under the presence of a solvent of chloroform, dichloromethane, tetrarhydrofurane, or acetonitrile.COPYRIGHT KIPO 2013본 발명은 9-히드록시-3-(2-히드록시에틸)-2-메틸-6,7,8,9-테트라히드로-4H- 피리도[1,2-a]피리미딘-4-온(화학식 1의 화합물)을 알킬설포닐 클로라이드 또는 아릴설포닐 클로라이드를 사용하여 선택적으로 클로로화하여 높은 수율로 9-히드록시-3-(2-클로로에틸)-2-메틸-6,7,8,9-테트라히드로-4H-피리도[1,2-a]피리미딘-4-온(화학식 2의 화합물)을 제조하는 방법을 제공한다.