Abstract: The present invention provides an efficient route to the C-13 side chain of the anti-cancer drug paclitaxel (TAXOL) and its analogs. The process includes the resolution of racemic erythro 2-hydroxy-3-amino-3-phenylpropionamide by diastereomeric crystallization and its conversion via various intermediates to the threo-ethylester and threo-methylester isomers.
Type:
Grant
Filed:
October 14, 1998
Date of Patent:
February 15, 2000
Assignee:
Chiragene, Inc.
Inventors:
Sowmianarayanan Ramaswamy, Venkat G. Reddy, Yalin Luo