Patent ID: 6784304
Filing Date: 2004-08-31
Classification: C07C,C07D,C07F

Abstract:
A method for the preparation of a compound of the following formula VI or salt thereof: whereR1 is hydrogen, arylcarbonyl, alkoxycarbonyl or alkylcarbonyl; R2 is aryl, heterocyclo or alkyl; and T is a taxane moiety directly bonded at C-13 of said moiety; comprising the steps of: (a) contacting a compound of the following formula III or salt thereof: â€ƒwhere R1 and R2 are as defined above; and R5 and R6 are (a) each independently alkyl; or (b) together with the carbon atom to which they are bonded, form a cycloalkyl, cycloalkenyl or heterocyclo group; with a compound of the following formula IV or salt thereof: HOâ€”Tâ€ƒâ€ƒ(IV), â€ƒwhere T is as defined above, in the presence of a coupling agent, to form a compound of the following formula V or salt thereof: â€ƒwhere R1, R2, R5, R6 and T are as defined above; and (b) contacting said compound of the formula V or salt thereof with a ring-opening agent, and, optionally, deprotecting one or more protected hydroxyl groups, to form said compound of the formula VI or salt thereof.