Two-step conversion of protected taxane ester to paclitaxel

摘要

The present invention relates to a method of producing paclitaxel from a protected coupled ester compound having a formula:wherein P1 is a hydrogenatable protecting group, comprising the steps of deprotecting the 7-O-position, 3'-N-position and 2'-O-position thereof in the presence of an acid to form a first intermediate compound having a formula:wherein HA is said acid, and benzoylating the first intermediate compound at the 3'-N-position thereby to produce paclitaxel.