Synthesis of Aliskiren

摘要

The present invention provides novel process for the preparation of renin inhibitor Aliskiren or its derivatives, and its pharmaceutically acceptable salts. The present invention also provides novel intermediates used in the preparation of Aliskiren.

主权项

1. A process for the preparation of Aliskiren or a pharmaceutically acceptable salt thereof comprising the steps of:
a) converting the cyano group of a compound of Formula-III into an amide group to give a compound of Formula-IV; wherein R1 is O(CH2)3OCH3, R2 is OMe; and R3 and R4 are CH(CH3)2; b) reducing the azide group of the compound of Formula-IV to form an amine group and isolating the resulting compound of Formula-Ia; and c) optionally converting the compound of Formula-Ia into a pharmaceutically acceptable salt.