An umpolung strategy for the C(sp3)‐H aminomethylation of 2‐methylindole has been developed using trifluoroacetic acid to induce the transformation, with aminals serving as precursors of iminium ion. Mechanistic studies have clearly shown that trifluoroacetic acid may play a pivotal role in this strategy. The utilization of readily available starting materials, mild reaction conditions, tolerance to complex functional groups, combine with yields of up to 98% and potential biological applications render this protocol applicable and useful for organic synthesis and medicinal chemistry.

中文翻译：

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三氟乙酸促进 2-甲基吲哚 umpolung 实现 c（sp3）-H 活化


已经开发了一种用于 2-甲基吲哚的 C（sp3）-H 氨基甲基化的 umpolung 策略，使用三氟乙酸诱导转化，其中胺醛作为亚胺离子的前体。机制研究清楚地表明，三氟乙酸可能在这种策略中起关键作用。利用现成的起始材料、温和的反应条件、对复杂官能团的耐受性，再加上高达 98% 的产量和潜在的生物学应用，使该方案适用于有机合成和药物化学。