Abstract
Efficient synthesis of N,O‐heterocyclic tetra‐substituted trifluoromethyl‐3,1‐benzoxazines via a transition‐metal‐catalyzed decarboxylative intramolecular cyclization was achieved. The decarboxylation of N‐benzoyl trifluoromethyl‐benzoxazinones generated the amide oxygen nucleophile, allowing a selective internal C1‐attack on Pd‐ or Cu‐coordinated zwitterions, affording medicinally attractive tetra‐substituted vinyl‐ or ethynyl‐trifluoromethyl‐3,1‐benzoxazines. This protocol can be applied to the synthesis of perfluoroalkyl‐ and non‐fluorinated 3,1‐benzoxazines.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have