Title - A PROCESS FOR OBTAINING AZD9291 ANILINE OR A SALT THEREOF

Abstract

Claim 1: A process for the preparation of AZD9291 or a pharmaceutically acceptable salt thereof, characterized in that it comprises: a) reacting AZD9291 nitrodiamine of formula (3) or a salt thereof with hydrogen, in the presence of a palladium(0) and / or platinum(0) catalyst, and in the presence of an acid, to form AZD9291 aniline of formula (1) or a salt thereof, wherein the reaction is carried out in the presence of water, or in the presence of a mixture of water and a water-miscible solvent; b) reacting the resulting AZD9291 aniline or a salt thereof with an activated acrylic acid derivative or precursor, and where necessary, treating with a base to form the compound AZD9291 of formula (2); and c) optionally, forming a pharmaceutically acceptable salt thereof.

Claims

1. A process for the preparation of AZD9291 aniline of formula (I) or a salt thereof, characterized in that it comprises: reacting AZD9291 nitrodiamine of formula (III) or a salt thereof (FORMULA) with hydrogen, in the presence of a palladium(0) and / or platinum(0) catalyst, and in the presence of an acid, to form AZD9291 aniline of formula (I) or a salt thereof (FORMULA), wherein the reaction is carried out in the presence of water, or in the presence of a mixture of water and a water-miscible solvent. 14 Claims follow