Enzymatic hydrolysis methods for the preparation of c-10 and...

C - Chemistry – Metallurgy – 12 – N

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C12N 9/14 (2006.01) C07D 305/14 (2006.01) C12N 1/20 (2006.01) C12N 9/18 (2006.01) C12P 17/02 (2006.01) C12Q 1/04 (2006.01) C12Q 1/24 (2006.01)

Patent

CA 2125726

ABSTRACT ENZYMATIC HYDROLYSIS METHODS FOR THE PREPARATION OF C-10 AND C-13 HYDROXYL-BEARING TAXANES, ENZYMATIC ESTERIFICATION METHOD FOR THE PREPARATION OF C-10 ACYLOXY-BEARING TAXANES, AND USE THEREOF IN THE PREPARATION OF C-13 ACYLOXY-BEARING TAXANES An enzymatic hydrolysis method, wherein one or more C-10 acyloxy-bearing taxanes are contacted with an enzyme or microorganism capable of hydrolyzing said acyloxy groups to hydroxyl groups. Also provided is an enzymatic esterification method, wherein one or more C-10 hydroxyl-bearing taxanes are contacted with an acylating agent and an enzyme or microorganism capable of esterifying said hydroxyl groups to form acyloxy groups. Further provided is an enzymatic hydrolysis method, wherein one or more C-13 acyloxy-bearing taxanes are contacted with an enzyme or microorganism capable of hydrolyzing said acyloxy groups to hydroxyl groups. The methods are especially useful for the preparation of compounds which may be employed as intermediates in the preparation of taxanes such as taxol.

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