Patent ID: 6768012
Filing Date: 2004-07-27
Classification: A61P,C07D

Abstract:
A process for the preparation of paclitaxel, which comprises the following steps:a) protection of the hydroxyls at the 7- and 10-positions of 10-deacetylbaccatine III (10-DAB III), â€ƒwherein -R&boxH;Râ€²-trichloracetyl, or Râ€²=-acetyl and R is selected from t-butoxycarbonyl and trichloracetyl, b) esterification of the hydroxyl at the 13-position with 3-phenyl-2-epoxypropionic acid c) removal of the protective groups at 7 and 10 (1) if they are both trichloroacetyl groups, followed by selective acetylation at the 10-position (2) and opening of the epoxide with sodium azide (3); â€ƒor, alternatively, câ€²) if Râ€²=acetyl and R=trichloroacetyl, opening of the epoxide with sodium azide and simultaneous deprotection at the 7-position d) reduction of the azido group to amino group e) benzoylation to give the final product