Eugenia Marqués‐López, Isaac G. Sonsona, Miryam Garcés‐Marín, M. Concepción Gimeno, Raquel P. Herrera

Asymmetric Organocatalyzed Phospha‐Michael Addition for the Direct Synthesis of Biologically Active Chromenylphosphonates

  • Organic Chemistry
  • Catalysis

AbstractThe potential of phosphites as nucleophiles for the asymmetric synthesis of chiral chromene derivatives has been overlooked in the literature. Herein, we report a promising approach via asymmetric organocatalyzed phospha‐Michael addition to iminochromenes, using a bifunctional squaramide, which gives access to chromenylphosphonates, an interesting family of bioactive compounds. Our optimized protocol provides very good reactivity, affording yields of up to 95% and with chiral products exhibiting an enantiomeric excess of up to 98%.

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