作者: Jerome Waser , Vincent Pirenne , Emma G. L. Robert
DOI: 10.1039/D1SC01127H
关键词: Indoline 、 Medicinal chemistry 、 Annulation 、 Diastereomer 、 Stereocenter 、 Chemistry 、 Donor acceptor 、 Acceptor 、 Catalysis
摘要: The efficient catalytic activation of donor–acceptor aminocyclopropanes lacking the commonly used diester acceptor is reported here in a (3 + 2) dearomative annulation with indoles. Bench-stable tosyl-protected aminocyclopropyl esters were converted into cycloadducts 46–95% yields and up to 95 : 5 diastereomeric ratio using amounts triethylsilyl triflimide. Tricyclic indoline frameworks containing four stereogenic centers including all-carbon quaternary obtained.