A Process For The Preparation Of Rivaroxaban

摘要

Described is an improved, industrially feasible and environmental friendly process for the preparation of Rivaroxaban. Also described are novel compounds which may be used as intermediates in preparation of Rivaroxaban.

主权项

1. A process for the preparation of Rivaroxaban (I) comprising: a) reacting a compound of formula (IV) with a compound G-L of formula (V), optionally in the presence of a suitable base to give a compound of formula (VI) wherein L is a leaving group and G is a protecting group; b) converting the compound of formula (VI) to a compound of formula (VII) or salt thereof which may optionally involve isolation of a compound of formula (VII′) c) reacting the compound of formula (VII) or salt thereof with 5-chloro thiophen-2-carboxylic acid of formula (VIII) in the presence of a suitable base to give a compound of formula (IX) wherein L1 is a leaving group; and d) deprotecting and cyclizing the compound of formula (IX) to provide Rivaroxaban (I).