A kind of preparation method of vinpocetine analog

A technique for vinpocetine and analogs, which is applied in the field of preparing vinpocetine analogs and achieves the effects of high yield, low impurity content and low price
CN103664941BInactive Publication Date: 2015-12-02HUNAN KEYUAN BIO PRODS
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HUNAN KEYUAN BIO PRODS
Publication Date
2015-12-02
Estimated Expiration
Not applicable · inactive patent

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Abstract

A preparation method of a vinpocetine analogue comprises the following steps: using UHP (urea hydrogen peroxide) for selective oxidation of a tabersonine analogue, then performing reduction, rearrangement, crystallization, and the like; or using the UHP for selective oxidation of a tabersonine reduction analogue (vinca-fuming analogue), then performing rearrangement, crystallization, and the like to obtain the vinpocetine analogue. Compared with the prior art, the preparation method has the advantages of high yield, direct quantification, simple operation, mild reaction conditions, suitability for industrial production, the yield reaching over 87%, more than 99% of HPLC (high performance liquid chromatography), a white product, good quality and low preparation cost.
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Description

technical field

[0001] The invention relates to a method for preparing vinpocetine analogues, belonging to the technical field of organic synthesis. Background technique

[0002] Vinpocetine analogs are an alkaloid that was first isolated from Vinca vinca by Zabolatnaya et al. in 1950. Its structural formula is as follows:

[0003]

[0004] In terms of structural formula, vinpocetine analogs belong to eburnamine-vincamine alkaloids (eburnamine-vincamine alkaloids), and are commonly found in plants of the family Apocynaceae in nature. Most compounds in this class of alkaloids have pharmacological activities on cell proliferation, cardiovascular, cerebrovascular and nervous system functions, which have aroused widespread interest of medicinal chemists.

[0005] In recent decades, many vincamine derivatives with higher biological activity and less toxic side effects than their parent natural products have been synthesized; the most famous one is apovincine ethyl ester, also...

Claims

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