首页> 外国专利> Preparation of C-10 and C-13 hydroxyl-containing taxanes by enzymatic hydrolysis, Preparation of C-10 acyloxy-containing taxanes by enzyme esterification, and Preparation of C-13 acyloxy-containing taxanes Their use in

Preparation of C-10 and C-13 hydroxyl-containing taxanes by enzymatic hydrolysis, Preparation of C-10 acyloxy-containing taxanes by enzyme esterification, and Preparation of C-13 acyloxy-containing taxanes Their use in

机译:酶水解法制备C-10和C-13羟基紫杉烷类;酶酯化法制备C-10酰基氧基紫杉烷类; C-13酰基氧基紫杉烷类的制备

摘要

The present invention relates to a method for enzymatic hydrolysis wherein at least one C-10 acyloxy-containing taxane is contacted with an enzyme or microorganism capable of hydrolyzing the acyloxy group with a hydroxyl group. The present invention also provides an enzymatic esterification process wherein one or more C-10 hydroxyl-containing taxanes are contacted with an acylating agent and an enzyme or microorganism capable of esterifying the hydroxyl group to form an acyloxy group. Also provided is an enzymatic hydrolysis method in which at least one C-13 acyloxy-containing taxane is contacted with an enzyme or microorganism capable of hydrolyzing the acyloxy group with a hydroxyl group. The methods of the present invention are particularly useful for the preparation of compounds that can be used as intermediates in the preparation of taxanes such as Taxol.
机译:本发明涉及一种酶促水解的方法,其中至少一种含C-10酰氧基的紫杉烷与能够水解带有羟基的酰氧基的酶或微生物接触。本发明还提供了一种酶促酯化方法,其中使一种或多种含C-10羟基的紫杉烷与酰化剂和能够使羟基酯化以形成酰氧基的酶或微生物接触。还提供了一种酶促水解方法,其中使至少一种含C-13酰氧基的紫杉烷与能够水解带有羟基的酰氧基的酶或微生物接触。本发明的方法对于制备可用作紫杉烷类如紫杉酚的中间体的化合物特别有用。

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