Patent ID: 6350887
Filing Date: 2002-02-26
Classification: A61P,C07D

Abstract:
A method for the preparation of a sidechain-bearing taxane of the following formula VII or a salt thereof: where the carbon atom marked with an asterisk is non-asymmetric;Bz is benzoyl: Ac is acetyl: R7 is hydrogen, alkylcarbonyl, or a hydroxyl protecting group; and R8 is hydrogen or a hydroxyl protecting group; comprising the step of contacting a &bgr;-lactam of the following formula I, which is (3R-cis)-1-benzoyl-3-(1-methoxy-1-methylethoxy)-4-phenyl-2-azetidinone: â€ƒwith a taxane compound of the following formula X: â€ƒwhere Bz, Ac, R7 and R8 are as defined above, or salts thereof, in the presence of a coupling agent; and optionally, converting the group â€”OC*(CH3)2(OCH3) of said compound of the formula VII to hydroxyl, thereby forming a sidechain-bearing taxane or a salt thereof of the following formula IX: â€ƒwhere Bz, Ac, R7 and R8 are as defined above.