Asymmetric Organocatalyzed Phospha-Michael Addition to Iminochromenes

23 May 2023, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


The potential of phosphites as nucleophiles for the synthesis of chiral chromene derivatives has been overlooked in the literature. Herein, we report a highly promising approach via asymmetric organocatalyzed phospha-Michael addition to iminochromenes, using a bifunctional squaramide. Our optimized protocol provides very good reactivity, affording yields of up to 95% and excellent enantioselectivity, with chiral products exhibiting an outstanding enantiomeric excess of up to 98%.




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