发明名称 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.
分类号 C07C271/22;C07D305/14;C07F7/18 主分类号 C07C271/22
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