Corynantheine-type alkaloids are major components of the Mitragyna speciosa, also known as kratom, that exhibit unique pharmacological activity. However, no universal method to prepare these alkaloids has been reported. Disclosed herein is a catalytic, asymmetric platform that enables rapid access to corynantheine alkaloids. The first enantioselective total synthesis of (−)-corynantheidine pseudoindoxyl is described. The first asymmetric syntheses of (+)-corynoxine and (−)-corynoxine B were also achieved, along with enantioselective syntheses of (−)-corynantheidol and (−)-corynantheidine. Through this work, all series of corynantheine alkaloids including indole, spirooxindole, and pseudoindoxyl can now be accessed in the laboratory, enabling comprehensive biological investigation of kratom alkaloids to be undertaken.

中文翻译：

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棒花青型棒花生物碱的合成平台

棒南茶碱型生物碱是帽柱木（也称为卡痛叶）的主要成分，具有独特的药理活性。然而，尚未报道制备这些生物碱的通用方法。本文公开的是能够快速获得棒南藤生物碱的催化不对称平台。描述了 (-)-corynantheidine 假吲哚酚的第一个对映选择性全合成。还实现了 (+)-corynoxine 和 (-)-corynoxine B 的首次不对称合成，以及 (-)-corynantheidol 和 (-)-corynantheidine 的对映选择性合成。通过这项工作，现在可以在实验室中获得包括吲哚、螺吲哚和假吲哚酚在内的所有系列的棒菊碱生物碱，从而能够对卡痛生物碱进行全面的生物学研究。