申请人:Hui Yongzheng
公开号:US20080275225A1
公开(公告)日:2008-11-06
A synthetic method of 20(s)-ginsenoside Rh2, that is 20(S)-protopanaxdiol-3-O-β-D-glucopyranoside, is comprised of: protecting protopanaxdiol (A1) selectively first to produce monosubstituted protopanaxdiol (A2); and Glycosidating the monosubstituted protopanaxdiol with Glucopyranosyl donor in the presence of Lewis acid catalyst; Deprotecting the product; Then separating and purifying to obtain 20(s)-ginsenoside Rh2. The method is conducted under mild condition at low cost, and affords product with high stereoselectivity, high yield and purity. Therefore, the synthetic method of the present invention is suitable for production on large scale.
一种20(s)-人参皂苷Rh2的合成方法,即20(S)-原人参二醇-3-O-β-D-葡萄糖苷,包括:首先选择性地保护原人参二醇(A1)以生成单取代原人参二醇(A2);然后在Lewis酸催化剂存在下将单取代原人参二醇与葡萄糖吡喃基供体进行糖苷化反应;脱保护产物;然后分离纯化以获得20(s)-人参皂苷Rh2。该方法在温和条件下,成本低廉,并且产物具有高立体选择性、高产率和纯度。因此,本发明的合成方法适用于大规模生产。