CAS: 142203-65-4; 13-Acetyl-9-Dihydrobaccatin Iii

该化合物是来自税务的化合物,特别是主要用于肿瘤学的帕利塔克斯和多塞沙勒半合成物的关键中间体. 巴卡廷三世的衍生物具有稳定的二氢结构和C-13位置的乙酰组,增强了其在受控合成改造中的效用.其高纯度和定义明确的立体化学使其对研究和制药生产具有价值,确保复杂的合成途径的产量一致.该化合物的结构完整性和与选择性功能化反应的兼容性有助于其作为首选的分类物合成前体的作用,支持抗舌体药物开发的进步.

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CAS号27548-93-2 巴卡丁III

合成工艺路线路线简述

    海关参考信息

    专利信息


    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.
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    主要参考文献


    1: Gunawardana, G.P., Premachandran, U., Burres, N.S., et al. Isolation of 9-Dihydro-13-acetylbaccatin III from Taxus canadensi. J. Nat. Prod. 55(11), 1686-1689 (1992).

    合成参考文献


    参考文献:10.5281/zenodo.5794106
    摘要:The LOTUS Initiative for Open Natural Products Research: frozen dataset union wikidata (with metadata) | DOI:10.5281/zenodo.5794106
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