专利号:WO-2024109742-A1 优先权日:2022-11-21 标题:Method for efficiently synthesizing bufadienolides and derivatives thereof 发明人:LIN GUOQIANG; YE WENBO; ZHAO QUNFEI; ZHANG JIANGE; HE QINGLI; WANG CHAO; YU SHAOPENG 权利人:UNIV SHANGHAI TRADITIONAL CHINESE MEDICINE 摘要:Disclosed in the present invention is a method for efficiently synthesizing bufadienolides and derivatives thereof. By starting from cheap and easily-available androstenedione 4-AD, the method performs bio-enzyme oxidization on same to obtain 14-α-hydroxy-androstane-17-one compounds, then completes loading of E-ring pyrone by using chemical conversion without any protective group so as to obtain a key intermediate, and achieves synthesis of bufadienolides by starting from the key intermediate. The method synthesizes resibufogenin in just eight operation steps, has simple and short route, simple operations and large reaction scale, can be used for large-scale preparation of such natural products, and has use prospects in industrial production.
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