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 |