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    Process for the preparation of 10-deacetylbaccatin III
    1.
    发明授权
    Process for the preparation of 10-deacetylbaccatin III 失效
    制备10-脱乙酰基浆果赤霉素III的方法

    公开(公告)号：US06437154B1

    公开(公告)日：2002-08-20

    申请号：US09963768

    申请日：2001-09-28

    Applicant: Sunil Kumar Chattopadhyay ,  Sachin Srivastava ,  Vijay Kumar Mehta

    Inventor： Sunil Kumar Chattopadhyay ,  Sachin Srivastava ,  Vijay Kumar Mehta

    IPC: C07D30514

    CPC classification number: C07D305/14

    Abstract: The present invention discloses a process for the conversion of a mixture of taxol analogues 7-xylosyl-10-deacetylbaccatin taxols of the formula 2 where R is C6H5, CH3C═CHCH3 or C5H11 into 10-deacetylbaccatin III of the formula 1 by dissolving the taxol analogue of formula 2 in a polar solvent, reacting the resultant solution with a base at a temperature of 20-50° C. for a time period in the range of 20-40 hours, and isolating 7-xyloxyl-10-deacetylbaccatin III, dissolving the 7-xylosyl-10-deacetylbaccatin III in a polar solvent, reacting the resultant solution with a periodate at 20-40° C. for a time period in the range of 20-40 hours to cleave the diol system of the xyloside into dialdehyde, treating the generated dialdehyde in an organic acid medium with salts of amine at 0-40° C. for 12-18 hours and isolating 10-deacetylbaccatin III of formula 1.

    Abstract translation: 本发明公开了一种将式2的紫杉醇类似物7-木糖基-10-脱乙酰基浆果赤霉素类紫杉醇的混合物，其中R为C6H5，CH3C = CHCH3或C5H11，转化为式1的10-脱乙酰基浆果赤霉素Ⅲ的方法， 式2在极性溶剂中，使所得溶液与碱在20-50℃的温度下反应20-40小时的时间，并分离7-木糖基-10-脱乙酰基浆果赤霉素III，将 7-木糖基-10-脱乙酰基浆果赤霉素III在极性溶剂中，使所得溶液与20-40℃的高碘酸盐反应20-40小时的时间段，将木糖苷的二醇体系切割成二醛， 在有机酸介质中用胺的盐在0-40℃处理生成的二醛12-18小时，并分离出式1的10-脱乙酰基浆果赤霉素III。

    Process for the production of a compound (+) catechin penta acetate useful as a precursor for the production of (+) catechin
    2.
    发明授权
    Process for the production of a compound (+) catechin penta acetate useful as a precursor for the production of (+) catechin 失效
    用于制备（+）儿茶素的化合物（+）儿茶素五乙酸酯的方法，其用作（+）儿茶素

    公开(公告)号：US06365757B1

    公开(公告)日：2002-04-02

    申请号：US09535767

    申请日：2000-03-28

    Applicant: Sunil Kumar Chattopadhyay ,  Suchitra Banerjee ,  Shipra Agarwal ,  Koneni Venkata Sashidhara ,  Vinayak Tripathi ,  Arun Kumar Kukreja ,  Sushil Kumar ,  Manish Kulshrestha ,  Ram Prakash Sharma ,  Vijay Kumar Mehta

    Inventor： Sunil Kumar Chattopadhyay ,  Suchitra Banerjee ,  Shipra Agarwal ,  Koneni Venkata Sashidhara ,  Vinayak Tripathi ,  Arun Kumar Kukreja ,  Sushil Kumar ,  Manish Kulshrestha ,  Ram Prakash Sharma ,  Vijay Kumar Mehta

    IPC: C07D31104

    CPC classification number: C07D311/60

    Abstract: This invention relates to a process for the production of a compound (+) catechin penta acetate of formula I from Taxus wallichiana tissue cultures which comprises : (a) inoculation of explants on different media compositions supplemented with combinations of auxins (1-5 mg/l) and cytokinins (0.1-1.0 mg/l); (b) incubation of the cultures under continuous light or dark conditions for 4-6 weeks for callus cultures followed by subculturing at 4-6 weeks intervals; (c) harvesting of the calli at different growth phases ranging from 12-36 months; (d) extraction of fresh pulverized calli with polar solvents at room temperature; (e) evaporating the solvent to give a residue; and partitioning of the residue between water and chlorinated solvents and evaporating the solvent to a semisolid mass; (f) subjecting the resultant mass to column chromatography over suitable adsorbent and (g) eluting with organic solvent/mixtures of organic solvents to get (+) catechin penta acetate.

    Abstract translation: 本发明涉及一种从紫杉属组织培养物生产式I化合物（+）儿茶素五乙酸酯的方法，该方法包括：（a）将外植体接种在不同的培养基组合物上，所述培养基组合物补充有生长素组合（1-5mg / l）和细胞分裂素（0.1-1.0mg / l）; （b）在连续的光照或黑暗条件下培养培养物4-6周，用于愈伤组织培养，然后以4-6周间隔传代培养; （c）在12-36个月的不同生长阶段收获愈伤组织; （d）在室温下用极性溶剂萃取新鲜的粉状愈伤组织; （e）蒸发溶剂得到残余物; 并将残留物在水和氯化溶剂之间分配并将溶剂蒸发成半固体物质; （f）使所得物质经合适的吸附剂进行柱层析，和（g）用有机溶剂/有机溶剂的混合物洗脱得到（+）儿茶素五乙酸酯。

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