Selective enzymatic esterification and solvolysis of epimeric vitamin D analog and separation of the epimers

A technology for epimers and vitamins, which is applied in the field of separation of mixed epimers of vitamin D analogues, and can solve problems such as difficult effective separation and close retention time
CN1639329AInactive Publication Date: 2005-07-13TEVA PHARMA IND LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
TEVA PHARMA IND LTD
Publication Date
2005-07-13
Estimated Expiration
Not applicable · inactive patent

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Abstract

Provided is a method of selectively enzymatically esterifying or selectively enzymatically solvolyzing epimers of analogs of vitamin D having a stereogenic center at C-24 that has a free or esterified OH group. The metod can be used, for example, for separating mixed epimers of the vitamin D analog.
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Description

field of invention

[0001] The present invention relates to methods for the selective enzymatic esterification and selective enzymatic solvolysis of the C-24 epimer of vitamin D analogues and esters thereof. The present invention further relates to a method of isolating mixed epimers of a vitamin D analog comprising a selective enzymatic esterification step or a selective enzymatic solvolysis step.

[0002] related application

[0003] This application claims priority to US Provisional Patent Application 60 / 348,082, filed January 10, 2002, and US Provisional Patent Application 60 / 349,977, filed January 18, 2002. Background of the invention

[0004] Since its discovery as vitamin D 3 The hormonally active metabolite form of 1α, 25-dihydroxyvitamin D 3 (1,25-(OH) 2 D. 3 ) Since then, many analogues have been prepared in order to obtain active substances with a hypocalcemic effect. Much effort has been devoted to the modification of the vitamin D side chain. While the 1α ...

Claims

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