PROCESS FOR PREPARATION OF DRONEDARONE BY GRIGNARD REACTION

摘要

The invention relates to a novel process for the preparation of dronedarone (I) and pharmaceutically acceptable salts thereof, which comprises reacting of compound of formula (IV) with compound of formula (VI) in a Grignard reaction, and the obtained product is isolated and, if desired, converted into a pharmaceutically acceptable salt thereof. The invention also relates to some novel intermediary compounds and processes for the preparation thereof.;

主权项

1. A process for the preparation of dronedarone (I) or a pharmaceutically acceptable salt thereof, comprising the steps of: a) reacting a compound of formula (IV) wherein X is Cl or Br, with a compound of formula (VI) or a salt thereof, in a Grignard reaction, wherein R is a group of formula —NR1R2,
wherein R1 and R2 are independently selected from the group consisting of H, alkyl, alkyloxy and aryl; b) isolating dronedarone (I); and c) optionally converting dronedarone (I) into a pharmaceutically acceptable salt thereof.