School of Chemistry, University of Hyderabad, Hyderabad 500046, Telangana, India.
J Org Chem. 2022 Aug 5;87(15):10359-10365. doi: 10.1021/acs.joc.2c00552. Epub 2022 Jul 12.
A metal-free method for the formylation/acylation of indoles and β-carbolines with (NH)SO via direct decarboxylative cross-coupling of α-oxo/ketoacids in moderate to good yields is described. The reaction occurs between ambient temperature and 40 °C under mild reaction conditions with commercially available starting materials. This methodology can be expanded to some biologically active indole alkaloids like pityriacitrins, eudistomins Y and Y, and marinacarbolines A-D.
本文描述了一种通过α-氧代/酮酸的直接脱羧交叉偶联，在温和条件下，（NH）SO 实现吲哚和β-咔啉的甲酰化/酰化的无金属方法，产率中等至良好。该反应在环境温度至 40°C 之间进行，使用市售起始原料，反应条件温和。这种方法可以扩展到一些具有生物活性的吲哚生物碱，如吡替拉嗪、依杜斯顿 Y 和 Y 以及海洋咔啉 A-D。
