（-）-雷奈酸酯的简洁对映选择性合成。
A concise enantioselective synthesis of (-)-ranirestat.
机构信息
Department of Chemistry, Stanford University, Stanford, California 94305, USA.
出版信息
Org Lett. 2010 Mar 19;12(6):1276-9. doi: 10.1021/ol100167w.
Abstract
A concise, enantioselective synthesis of the potent aldose reductase inhibitor ranirestat (1) is reported. The synthesis was accomplished employing inexpensive, commercially available starting materials. A palladium-catalyzed asymmetric allylic alkylation (Pd-AAA) of malonate 4 was utilized as a key transformation to construct the tetrasubstituted chiral center in the target.
摘要
报道了一种强效醛糖还原酶抑制剂瑞那司他（1）的简洁、对映选择性合成方法。该合成采用了廉价、市售的起始原料完成。利用钯催化的不对称烯丙基烷基化（Pd-AAA）反应，将丙二酸酯 4 作为关键转化步骤，构建目标分子中的四取代手性中心。
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