INTERMEDIATE COMPOUND FOR PRODUCING PACLITAXEL AND METHOD OF PRODUCING THE SAME
摘要
1. An intermediate compound for producing paclitaxel wherein the intermediate compound having the general formula wherein P1 is a hydrogenatable benzyl protecting group. 2. A paclitaxel intermediate compound according to claim 1 wherein the hydrogenatable benzyl protecting group is selected from a group consisting of benzyloxymethyl and benzyl. 3. A process for the preparation of a paclitaxel intermediate compound wherein the intermediate compound having the general formula wherein P1 is a hydrogenatable benzyl protecting group comprising the condensation of a compound having the formula wherein P1 is a hydrogenatable benzyl protecting group with C7 TES-protected baccatin III of the formula 4. A process according to claim 3 wherein the condensation is conducted in the presence of a dialkyl carbodiimide. 5. A process according to claim 4 wherein said dialkyl carbodiimide is selected from a group consisting of diisopropylcarbodiimide and dicyclohexyl carbodiimide. 6. A process according to claim 5 wherein said dialkyl carbodiimide is diisopropylcarbodiimide and said condensation is conducted in the presence of dimethylamino pyridine in toluene. 7. A process according to claim 6 wherein the condensation is conducted at a temperature of about 80 degree C for a time interval of three to five hours. 8. A process according to claim 3 wherein the condensation is conducted n the presence of dialkyl carbodiimide and dimethylamino pyridine in toluene at a temperature of about 80 degree C for a time interval of three to five hours. 9. A process according to claim 8 wherein said dialkyl carbodiimide is selected from a group consisting of diisopropylcarbodiimide and dicyclohexyl carbodiimide. 10. A process according to claim 9 wherein diisopropylcarbodiimide is used as dialkyl carbodiimide.
申请公布号
EA000678(B1)
申请公布日期
2000.02.28
申请号
EA19980000024
申请日期
1996.06.07
申请人
NAPRO BIOTHERAPEUTICS, INC.;BRYN MAWR COLLEGE
发明人
SISTI, NICHOLAS, J.;SWINDELL, CHARLES, S.;CHANDER, MADHAVI, C.