BABU, Srinivasan,CHENG, Zhigang,GOSSELIN, Francis,HIDBER, Pirmin,HOFFMANN, Ursula,HUMPHRIES, Theresa,REENTS, Reinhard,TIAN, Qingping,YAJIMA, Herbert
申请号：
ES13774174
公开号：
ES2594078T3
申请日:
2013.10.09
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A process for preparing (S) -1- (4 - ((2- (2-aminopyrimidin-5-yl) -7-methyl-4-morpholinothiene [3,2-d] pyrimidin-6- yl) methyl) piperazin -1-yl) -2-hydroxypropan-1-one I, which has the structure: ** Formula ** and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, comprising: (a) reacting a (S) -2-hydroxy-1- (piperazin-1-yl) propan-1-one 6 and 2-chloro-7-methyl-4-morpholinothiene [3,2-d] pyrimidine-6-carbaldehyde IV salt with a reducing agent to give (S) -1- (4 - ((2-chloro-7-methyl-4- morpholinothiene [3,2-d] pyrimidin-6-yl) methyl) piperazin-1-yl) - 2-hydroxypropan-1-one II ** Formula ** and (b) react II, a palladium catalyst, and 2-aminopyrimidin-5-ylboronic acid III having the structure: ** Formula ** to give I.Un proceso para preparar (S)-1-(4-((2-(2-aminopirimidin-5-il)-7-metil-4-morfolinotieno[3,2-d]pirimidin-6- il)metil)piperazin-1-il)-2-hidroxipropan-1-ona I, que tiene la estructura:**Fórmula** y estereoisómeros, isómeros geométricos, tautómeros, y sales farmacéuticamente aceptables de la misma, que comprende: (a) hacer reaccionar una sal de (S)-2-hidroxi-1-(piperazin-1-il)propan-1-ona 6 y 2-cloro-7-metil-4- morfolinotieno[3,2-d]pirimidina-6-carbaldehído IV con un agente reductor para dar (S)-1-(4-((2-cloro-7-metil-4- morfolinotieno[3,2-d]pirimidin-6-il)metil)piperazin-1-il)-2-hidroxipropan-1-ona II**Fórmula** y (b) hacer reaccionar II, un catalizador de paladio, y ácido 2-aminopirimidin-5-ilborónico III que tiene la estructura:**Fórmula** para dar I.
