首页> 外国专利> Preparation of 10-deacetylbaccatin III and 7-protected-10- deacetylbaccatin III derivatives from 10-deacetyl taxol A, 10-deacetyl taxol B, and 10-deacetyl taxol C

Preparation of 10-deacetylbaccatin III and 7-protected-10- deacetylbaccatin III derivatives from 10-deacetyl taxol A, 10-deacetyl taxol B, and 10-deacetyl taxol C

机译:由10-去乙酰基紫杉醇A,10-去乙酰基紫杉醇B和10-去乙酰基紫杉醇C制备10-去乙酰基浆果赤霉素III和7-保护的-10-去乙酰基浆果赤霉素III衍生物

摘要

The present invention relates to a process for converting purified, partially purified or crude taxane mixtures into a protected precursor of 10-deacetylbaccatin III and into 10-deacetylbaccatin III. The process comprises three steps, the first of which includes contacting a mixture containing at least one naturally occurring taxane compound having the structure (II) ##STR1## in which R.sub.1 is phenyl, ##STR2## [an ester linkage at the C-13 position] with at least one hydroxy protecting group. The second step involves cleaving the ester linkage of the protected taxane thus giving rise to a protected precursor of 10- deacetylbaccatin III, the deprotection of which leads to 10- deacetylbaccatin III.
机译:本发明涉及将纯化的,部分纯化的或粗制的紫杉烷混合物转化成受保护的10-脱乙酰浆果赤霉素III前体和10-脱乙酰浆果赤霉素III的方法。该方法包括三个步骤,其中第一步包括使含有至少一种天然紫杉烷化合物的混合物接触,该化合物具有结构(II)## STR1 ##,其中R1是苯基,## STR2 ## [在C-13位的酯键]具有至少一个羟基保护基。第二步涉及裂解被保护的紫杉烷的酯键,从而得到10-脱乙酰基浆果赤霉素III的被保护的前体,其去保护基团导致10-脱乙酰基浆果赤霉素III。

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