发明名称 |
PROCESS FOR SYNTHESISING BROMINATED ENEYNE COMPOUND E, E-22-BROMO-9,11,19-TRIYNE-17,21-DIENE DOCOSANOIC ACID ESTER |
摘要 |
<p>The present invention relates to a process for synthesising a long-chain brominated eneyne compound E-22-bromo-9,11,19-triyne-17,21-diene docosanoic acid ester which is active in reducing fat and weight and has the following formula. The process comprises: a. bromizing a compound of formula 2 with NBS under the effect of silver nitrate to produce a compound of formula 3; b. reacting the compound of formula 3 with 6-heptyn-1-ol under the effect of an amine, a cuprous compound and hydroxylamine hydrochloride to produce a compound of formula 4; c. oxidizing the compound of formula 4 with an oxidant to obtain a compound of formula 5; d. reacting the compound of formula 5 with trimethylsilylacetylene methyltriphenylphosphonium bromide under the effect of a base to obtain a compound of formula 6; e. de-protecting the compound of formula 6 under the effect of a fluorine agent to obtain a compound of formula 7; f. reacting the compound of formula 7 with 1,2-dibromoethylene under the catalysis of a cuprous compound, a palladium agent and an amine to obtain the compound of formula I. The synthesis process provided in the present invention is a novel synthetic route and easy to operate.</p> |
申请公布号 |
WO2014040476(A1) |
申请公布日期 |
2014.03.20 |
申请号 |
WO2013CN81762 |
申请日期 |
2013.08.19 |
申请人 |
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES |
发明人 |
GUO, YUEWEI;WANG, HEYAO;GONG, JINGXU |
分类号 |
C07C69/65;A61K31/201;A61P3/04;C07C51/43 |
主分类号 |
C07C69/65 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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