发明名称 Process for Preparing Quinoline Derivatives
摘要 A process for preparing a compound of Formula I is disclosed, comprising the steps:;;wherein: R1 is halo;R2 is halo;R3 is (C1-C6)alkyl or (C1-C6)alkyl optionally substituted with heterocycloalkyl;R4 is (C1-C6)alkyl; andQ is CH or N; comprising: (a) contacting 1,1-cyclopropane dicarboxylic acid with thionyl chloride in a polar aprotic solvent;(b) adding;;and a tertiary amine base to the mixture of step (a) to form a compound of Formula A; and;(c) coupling a compound of Formula A with an amine of Formula B to form a compound of Formula I.;
申请公布号 US2014256938(A1) 申请公布日期 2014.09.11
申请号 US201214353251 申请日期 2012.10.22
申请人 Exelixis, Inc. 发明人 Wilson Jo Ann;Naganathan Sriram;Andersen Neil G.;Pfeiffer Matthew
分类号 C07D215/233;C07C231/02 主分类号 C07D215/233
代理机构 代理人
主权项 1. A processes for preparing a compound of Formula A: wherein R2 is H, F, Cl, or Br;comprising (a) contacting 1,1-cyclopropane dicarboxylic acid with thionyl chloride in a polar aprotic solvent; and (b) addingand a tertiary amine base to mixture of step (a).
地址 South San Francisco CA US