PROCESS FOR PREPARATION OF FINGOLIMOD

摘要

The present invention provides a process for preparation of fingolimod, a compound of Formula I or a pharmaceutically acceptable salt thereof, free of regioisomeric impurity compound of Formula IA;

主权项

1. A process for preparation of fingolimod, a compound of Formula I or a pharmaceutically acceptable salt thereof, free of regioisomeric impurity compound of Formula IA comprising:
a. reacting a compound of Formula II with octanoyl halide to obtain a reaction mixture comprising a compound of Formula III and its corresponding regioisomer a compound of Formula IIIA; b. hydrolyzing the reaction mixture resulting from step ‘a’ to obtain a reaction mixture comprising a compound of Formula IV and its corresponding regioisomer a compound of Formula IVA; and isolating the compound of Formula IV which is free of its regioisomeric impurity compound of Formula IVA; c. converting the compound of Formula IV resulting from step ‘b’ to a compound of Formula III by subjecting to acetylation;d. converting the compound of Formula III to a compound of Formula VI by subjecting to reduction and deacetylation; e. converting the compound of Formula VI to a compound of Formula IX; and f. converting the compound of Formula IX to fingolimod, compound of Formula I or pharmaceutically acceptable salt thereof.