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Updated: Dec 18, 2025

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Asymmetric alkynylation/lactamization cascade: an expeditious entry to enantiomerically enriched isoindolinones
Vishnumaya Bisai1, Arun Suneja, Vinod K Singh
1Department of Chemistry, Indian Institute of Science Education and Research Bhopal, Bhopal, M.P. - 462 066 (India); Indian Institute of Technology, Kanpur, U.P. - 208 016 (India).
Abstract:
An unprecedented Cu(I)-pybox-diPh-catalyzed highly enantioselective (up to >99% ee) alkynylation/lactamization cascade has been developed as a general catalytic system for the synthesis of diversely substituted isoindolinones of immense biological importance. The cascade effects one C-C and two C-N bond-forming events in one reaction vessel under operationally simple, additive-free reaction conditions in good to excellent yields. The methodology was further extended to the synthesis of tetrahydroisoquinoline scaffolds common to several biologically active natural products in a two-step sequence with remarkable selectivity (up to 94% ee).
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