A chemo- and enantioselective protocol for the N-alkylation of indoles with imines was developed. This process was catalyzed by a BINOL-derived phosphoric acid catalyst to give the corresponding acyclic aminals of indoles in 46–99% yields with 70–98% ee. The application of this method for the “late-stage” functionalization of a bioactive compound was performed with high efficency. The products showed good stability and enabled many further transformations.

中文翻译：

---

手性磷酸催化的吲哚与亚胺的化学和对映选择性 N-烷基化

开发了用亚胺对吲哚进行 N-烷基化的化学和对映选择性方案。该过程由 BINOL 衍生的磷酸催化剂催化，以 46-99% 的产率和 70-98% ee 得到相应的吲哚无环缩醛胺。该方法用于生物活性化合物“后期”功能化的应用效率很高。产品表现出良好的稳定性，并可以进行许多进一步的转化。