Two-step conversion of protected taxane ester to paclitaxel

   
   

The present invention relates to a method of producing paclitaxel from a protected coupled ester compound having a formula: ##STR1## wherein P.sub.1 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: ##STR2## wherein HA is said acid, and benzoylating the first intermediate compound at the 3'-N-position thereby to produce paclitaxel.

A invenção atual relaciona-se a um método de produzir o paclitaxel de um composto acoplado protegido do ester que tem uma fórmula: ## do ## STR1 wherein P.sub.1 é um grupo protegendo hydrogenatable, compreendendo as etapas de deprotecting o 7-O-position, 3'-N-position e 2'-O-position disso na presença de um ácido para dar forma a um primeiro composto intermediário que tem uma fórmula: ## do ## STR2 wherein o HA é ácido dito, e benzoylating o primeiro composto intermediário no 3'-N-position desse modo para produzir o paclitaxel.

 
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