紫杉醇置于tetrabutylammonium Borohydride体系中,用 二氯甲烷 用作溶剂,化学反应 1.0H,以97%的收率获得巴卡丁 Iii 参考文献:Modified Taxols. 3. Preparation And Acylation Of Baccatin Iii 标题:Modified Taxols. 3. Preparation And Acylation Of Baccatin Iii 摘要: Doi:10.1021/jo00366A043
专利号:US-8293930-B1 优先权日:2004-06-25 标题 :One pot synthesis of taxane derivatives and their conversion to paclitaxel and docetaxel 发明人:NAIDU RAGINA 权利人:NAIDU RAGINA; CHATHAM BIOTEC LTD 摘要:A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediate in a one pot reaction of protecting the C-7 and C-10 positions and attaching a side chain at the C-13 position and subsequently deprotecting the group to form paclitaxel or docetaxel, and taxane intermediates.
专利号:US-7893283-B2 优先权日:2004-06-04 标题:Semi-synthesis of taxane intermediates and their conversion to paclitaxel and docetaxel 发明人:NAIDU RAGINA 权利人:CHATHAM BIOTEC LTD 摘要:A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediates.
专利号:US-6576777-B2 优先权日:1996-10-18 标 题:Semi-synthesis of a protected baccatin III compound 发明人:ZAMIR LOLITA; CARON GAETAN 权利人:INST NAT RECH SCIENT 摘要:The present invention relates to a semi-synthetic process to convert a naturally occurring taxane into a suitable starting material for the synthesis of paclitaxel and related compounds. Specifically, the present invention relates to a process for the conversion of 9-dihydro-13-acetylbaccatin III into a 7-protected baccatin III which can then be used as starting material for the synthesis of taxane derivatives such as paclitaxel, docetaxel, cephalomannine and other taxanes structurally related to baccatin III. The method as described uses a preparative scale technique which is amenable to commercial scale-up.
专利号:WO-2008032104-A1 优先权日:2006-09-15 标题:One pot synthesis of taxane derivatives and their conversion to paclitaxel and docetaxel 发明人:WALKER ROSS THOMSON; NAIDU RAGINA 权利人:CHATHAM BIOTEC LTD; WALKER ROSS THOMSON; NAIDU RAGINA 摘要:A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediate in a one pot reaction, of protecting the C-10 and attaching a side chain at C-13 position and subsequently deprotecting the group to form paclitaxel or docetaxel, and intermediates used therein.
专利号:WO-0134589-A1 优先权日:1999-11-05 标 题 :Semi-synthesis of baccatin iii from 9-dihydro-13-acetylbaccatin iii 发明人:ZAMIR LOLITA 权利人:ZAMIR LOLITA 摘要:The present invention relates to a semi-synthetic process to convert a naturally occurring taxane into a suitable starting material for the synthesis of paclitaxel and related compounds. Specifically, the present invention relates to a process for the conversion of 9-dihydro-13-acetylbaccatin III into baccatin III which can then be used as starting material for the synthesis of taxane derivatives such as paclitaxel, docetaxel, cephalomannine and other taxanes structurally related to baccatin III.
专利号:US-2005192445-A1 优先权日:2004-03-01 标题:Semi-synthesis of taxane intermediates and aziridine analogues and their conversion to paclitaxel and docetaxel 发明人:NAIDU RAGINA 权利人:PHYTOGEN LIFE SCIENCES INC 摘要:A process is provided for the semi-synthesis of taxane intermediates and aziridine analogues of cephalomannne and baccatin III intermediates, and the conversion of such intermediates and analogues to paclitaxel and docetaxel.
参考标题:Total Synthesis Of Baccatin Iii And Taxol 作者:Samuel J. Danishefsky,John J. Masters,Wendy B. Young,J. T. Link,Lawrence B. Snyder,Thomas V. Magee,David K. Jung,Richard C. A. Isaacs,William G. Bornmann,Cheryl A. Alaimo,Craig A. Coburn,Martin J. Di Grandi |发布日期:1996.1.1 摘要:An Intramolecular Heck Reaction (90 -> 91) Serves As The Key Step In The Total Synthesis Of The Titled Compounds. The Synthetic Route Is Based On Utilizing The Wieland−miescher Ketone (5) As A Matrix To Provide The C And D Rings Of The Targets And To Provide Functionality Implements For Joining This Sector To An A Ring Precursor (6). Catalytically Induced Enantiotopic Control And Early Emplacement Of
合成参考文献
摘要:White, J. D.; Carter, R. G., Science of Synthesis, (2002) 4, 398.