Oleanolic acid derivative, and preparation method and purpose thereof

A technology for oleanolic acid derivatives, applied in the field of preparation of oleanolic acid derivatives or pharmaceutically acceptable salts thereof, can solve the problems of low reactivity, high price, inflammability and explosion, and achieve The effect of high reaction yield, low production cost and mild reaction conditions
CN102070697AInactive Publication Date: 2011-05-25CHINA PHARM UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
CHINA PHARM UNIV
Publication Date
2011-05-25
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to the field of medicine, in particular to an oleanolic acid derivative shown as a formula I, and pharmaceutically acceptable salts, a preparation method and purpose thereof. The invention also discloses application of the compound shown by the formula I to the preparation of anti-tumor medicine of 2-cyano-3, 12-dioxo oleanane-1, 9(11)-diene-28-carboxylic acid (XI, CDDO), 2-cyano-3, 12-dioxo oleanane-1, 9(11)-diene-28-carboxylic imidazole (XIII, CDDO-Im) and 2-cyano-3, 12-dioxo oleanane-1, 9(11)-diene-28-carboxyl methylamine (XIV, CDDO-MA).
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Description

technical field

[0001] The present invention relates to the field of medicine, in particular to an oleanolic acid derivative represented by formula (I) or a pharmaceutically acceptable salt thereof, and a preparation method thereof. The present invention still further relates to the compound shown in formula (I) in preparing antitumor drug 2-cyano group-3,12-dioxooleanane-1,9(11)-diene-28-carboxylic acid ( CDDO), 2-cyano-3,12-dioxooleanane-1,9(11)-diene-28-carboxyimidazole (CDDO-Im) and 2-cyano-3,12- Application in dioxooleanane-1,9(11)-diene-28-carboxamide (CDDO-MA). Background technique

[0002] Oleanane-type (oleanane) pentacyclic triterpenoids represented by oleanolic acid (OA) are ubiquitous in nature and have a wide range of biological activities (Neoplasma, 2004, 51, 327-333), The optimization and derivation based on the structure of these natural compounds is one of the hotspots in the research of natural medicinal chemistry.

[0003]

[0004] 2-cyano-3,12-diox...

Claims

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