2'-O-Tert-Butyldimethylsilyl-7-O-Triethylsilyldocetaxel置于双氧水,碳酸氢钠,氟化氢吡啶体系中,用 四氢呋喃 用作溶剂,化学反应 18.0H,反应生成多西他赛 参考文献:A Facile N-Debenzoylation Of Paclitaxel: Conversion Of Paclitaxel To Docetaxel 标题:A Facile N-Debenzoylation Of Paclitaxel: Conversion Of Paclitaxel To Docetaxel 摘要:An Efficient And Regioselective Method For The N-Debenzoylation Of Paclitaxel Has Been Developed,And Has Been Applied To The Conversion Of Paclitaxel To 10-Acetyldocetaxel And To Docetaxel. (C) 1998 Elsevier Science Ltd. All Rights Reserved. Doi:10.1016/s0040-4039(98)02221-7
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-7202370-B2 优先权日:2003-10-27 标 题 :Semi-synthesis of taxane intermediates from 9-dihydro-13-acetylbaccatin III 发明人:NAIDU RAGINA 权利人:CONOR MEDSYSTEMS INC 摘要:A method is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel from 9-dihydro-13-acetylbaccatin III. The preparation of a suitably protected baccatin III backbone from 9-dihydro-13-acetylbaccatin III, and the insertion of the phenylisoserine side chain onto the protected baccatin III from 9-dihydro-13-acetylbaccatin III to form the taxane derivatives, paclitaxel and docetaxel is disclosed.
1: Conry RM. Response of follicular dendritic cell sarcoma to gemcitabine and docetaxel: report of two cases and literature review. Clin Sarcoma Res. 2014 Jun 28;4:6. doi: 10.1186/2045-3329-4-6. eCollection 2014. [Epub ahead of print] doi: 10.1016/j.ijpharm.2014.06.058. [Epub ahead of print]
合成参考文献
摘要:Taomoto J, Tanabe K, Suzuki T, Hamai Y, Emi M, Hihara J, Yoshida K, Okada M. [Adjuvant surgery for advanced gastric cancer]. Gan To Kagaku Ryoho. 2010 Feb;37(2):263–6. 摘要:Yanagisawa S, Tsuchiya S, Kaiho T, Togawa A, Shinmura K, Okamoto R, Nishimura M, Nomura S, Nobumoto D, Miyazaki M. [Histological complete response in a case of primary squamous cell carcinoma of the stomach treated by chemotherapy with docetaxel and cisplatin plus 5-fluorouracil]. Gan To Kagaku Ryoho. 2010 Feb;37(2):307–10. 参考文献:10.1245/s10434-010-0952-0 摘要:Gimbergues P, Dauplat MM, Durando X, Abrial C, Le Bouedec G, Mouret-Reynier MA, Cachin F, Kwiatkowski F, Tchirkov A, Dauplat J, Penault-Llorca F. Intraoperative Imprint Cytology Examination of Sentinel Lymph Nodes After Neoadjuvant Chemotherapy in Breast Cancer Patients. Annals of Surgical Oncology. 2010 Feb 13;17(8):2132–7. doi: 10.1245/s10434-010-0952-0. 参考文献:10.1097/01.mlg.0000177456.90870.94 摘要:Yoo GH, Lin HS, Iskander AJ, Piechocki MP, Oliver J, Kewson D, Lonardo F, Tainsky MA, Kim HR, Kim H, Ensley JF. Docetaxel associated pathways in cisplatin resistant head and neck squamous cell carcinoma: a pilot study. Laryngoscope. 2005 Nov;115(11):1938–46. doi: 10.1097/01.mlg.0000177456.90870.94. 参考文献:10.1007/s12094-010-0474-z 摘要:Gutiérrez-Gutiérrez G, Sereno M, Miralles A, Casado-Sáenz E, Gutiérrez-Rivas E. Chemotherapy-induced peripheral neuropathy: clinical features, diagnosis, prevention and treatment strategies. Clinical and Translational Oncology. 2010 Feb 20;12(2):81–91. doi: 10.1007/s12094-010-0474-z.