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    • 5. 发明授权
    • Method for the production of baccatin-III by enzymatic synthesis
    • 通过酶合成制备浆果赤霉素Ⅲ的方法
    • US06458568B1
    • 2002-10-01
    • US09311084
    • 1999-05-13
    • Konrad GlundMatthias HoffmannWolfram WeckwerthRainer Zocher
    • Konrad GlundMatthias HoffmannWolfram WeckwerthRainer Zocher
    • C12P1702
    • C12P17/02
    • A method for the continuous synthesis of baccatin-III is performed by means of the enzymatic acetylations of 10-deacetyl baccatin-III (10-DAB) in an enzyme reactor. This objective is accomplished by a method, for which an aqueous reaction batch is used, which contains a partially purified or a very pure acetyl transferase from a Taxus species and synthesis components, especially 10-DAB, acetyl compounds or optionally an acetyl coenzyme A, which can be regenerated, a protective colloid and optionally a buffer substance in solution. The solution is separated by a semipermeable membrane from an organic solvent, which serves as extraction agent for baccatin-III, the reaction batch being regenerated at regular intervals in an aqueous buffer system and the solvent continuously being exchanged. By conducting the reaction, the product can be removed continuously from the reaction batch for the partial synthesis of taxol and taxoter. By the above method, achievable yields are increased significantly.
    • 通过酶反应器中10-脱乙酰浆果赤霉素III(10-DAB)的酶促乙酰化进行浆果赤霉素III的连续合成方法。 该目的通过一种使用含水反应批料的方法来实现,该方法含有来自紫杉属物种和合成成分,特别是10-DAB,乙酰化合物或任选的乙酰辅酶A的部分纯化或非常纯的乙酰转移酶, 其可以再生,保护胶体和任选的溶液中的缓冲物质。 将溶液由半透膜与有机溶剂分离,其用作浆果赤霉素III的提取剂,反应批次在水性缓冲体系中以规则的间隔再生,溶剂连续交换。 通过进行反应,可以从反应批料中连续除去产物以部分合成紫杉醇和紫杉醇。 通过上述方法,可实现的产率显着增加。