A catalytic asymmetric [3 + 3] annulation of aziridines with substituted 2-vinylindoles was developed. The reaction proceeds through copper-catalyzed ring-opening of aziridines followed by base-promoted intramolecular aza-Michael addition in a one-pot process. This strategy provides an efficient method for the direct synthesis of 1,4-disubstituted tetrahydro-β-carbolines with generally high diastereo- and enantioselectivities (up to >20 : 1 dr, 96% ee).

中文翻译：

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铜（I）催化的涉及氮丙啶的不对称[3 + 3]环化反应，以构建四氢-β-咔啉

开发了具有取代的2-乙烯基吲哚的氮丙啶催化不对称[3 + 3]环。该反应通过铜催化的氮丙啶的开环进行，然后通过一锅法进行碱促进的分子内氮杂-Michael加成反应。该策略提供了一种直接合成具有高非对映选择性和对映选择性（最高> 20：1 dr，96％ee）的1,4-二取代的四氢-β-咔啉的有效方法。