An organocatalytic asymmetric formal aza‐[3+3]cycloaddition of readily available N‐Tosyl‐3‐aminobenzofuran with α,β‐unsaturated aldehydes was developed for the first time. This method enables the facile synthesis of biologically active and synthetically challenging polysubstituted fused benzofuran derivatives bearing two stereocenters in high yields with excellent diastereo‐, and enantioselectivity (up to >20 : 1 dr, and >99% ee).

中文翻译：

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3-氨基苯并呋喃与α，β-不饱和醛的有机催化不对称形式Aza- [3 + 3]环加成反应

首次开发了易于获得的N -Tosyl-3-氨基苯并呋喃与α，β-不饱和醛的有机催化不对称形式氮杂[3 + 3]环加成反应。该方法可以轻松合成具有两个立体中心的具有生物活性和合成挑战性的多取代稠合苯并呋喃衍生物，并具有出色的非对映选择性和对映选择性（高达> 20：1 dr，且> 99％ee）。