Processes for the Preparation of Axitinib,申请号US201615139494-传众专利搜索

Processes for the Preparation of Axitinib

申请公布号：US2016318898(A1)

申请号：US201615139494

申请日期：2016.04.27

申请公布日期：2016.11.03

申请人：

Signa S.A. de C.V.

发明人：Granados-Covarrubias Evin Hazael;Lazcano-Seres José Miguel;Melgar-Fernández Roberto Carlos;Zambrano-Huerta Armando;Montiel-Pérez Martín Raúl;Flores-García Israel

分类号：C07D401/06

主分类号：C07D401/06

地址：Toluca MX

摘要：Processes for the preparation of Axitinib in good yield (generally greater than 80%) are provided that avoid the use of a palladium-catalyzed coupling reaction.

主权项：1. A process for the preparation of a compound of Formula (1):the process comprising: (i) coupling, in the presence of a first base, a copper (I) catalyst and a ligand in a first solvent, a compound of Formula (2):with a compound of Formula (3):thereby forming a compound of Formula (4):and (ii) converting the compound of Formula (4) to Axitinib.