Formamide CH bond activation has been achieved under oxidative conditions, using a copper catalyst and tert‐butyl hydroperoxide (TBHP) as the external oxidant (see scheme). This oxidative coupling of a range of dialkyl formamides provides an easy, phosgene‐free route for the selective synthesis of Z‐enol carbamates and 2‐carbonyl‐substituted phenol carbamates in high yields.

This communication describes a catalystfree synthesis of 2-substituted quinazolines and 4H-]oxazines using commericially available sodium hypochlorite as oxidant. Operational simplicity, mild reaction conditions and the ability to construct structurally diverse 2-quinazolines and 2- ,3]oxazines by this method render it to be a practical alternative for the synthesis of these heterocycles.

A simple and elegant method for benzylic activation was demonstrated employing the potassium iodide/tert-butyl hydrogen peroxide catalytic system. This methodology was further extended for the synthesis of biologically important heterocycles namely, 3H-quinazolin-4-ones and 4H-3,1-benzoxazin-4-ones including mecloqualone and etaqualone which are important quinazolinone-based drugs used for the treatment of insomnia in good yields.

Die Aktivierung von Formamid‐C‐H‐Bindungen gelang unter oxidativen Bedingungen mit einem Kupferkatalysator und tert‐Butylhydroperoxid (TBHP) als externem Oxidationsmittel (siehe Schema). Diese mit hohen Ausbeuten verlaufende oxidative Kupplung einer Vielzahl an Dialkylformamiden bietet einen einfachen, phosgenfreien Zugang zu Z‐Enolcarbamaten und 2‐carbonylsubstituierten Phenolcarbamaten.

Direct access to unsymmetrical urea derivatives via copper catalysed C-H/N-H coupling of formamides with amines has been developed at room temperature. This protocol is also applied to the synthesis of chiral urea derivatives.