Oxidation Of 2-substituted Indole Synthesis Of Benzo Oxazine Research Ketones

Benzoxazinones are one of the most important fused nitrogen-containing heterocycles, which are commonly encountered in the structure of natural products and biologically active compounds. They are crucial precursors for the synthesis of bionts, pharmaceuticals, chemical dyes, spices, fungicides and herbicides. In addition, they are also versatile building blocks in organic synthesis and medicinal chemistry. Therefore, the methods for the synthesis of benzoxazinones have received intensive attention over the past decade. However, the current existing methods need acyl chlorides, peracids, carbon monoxide, or a noble metal catalyst, which are not easy to obtain, corrosive or hazardous materials. Therefore, the development of green and efficient, atom-economical, simple and readily available substrates, efficient functional group tolerance, and the large-scale methods still remain highly desirable for the organic chemists.The selective oxidation is very important for organic transformations. Particularly, oxidation reactions that utilize environmentally benign oxidants have been and continue to be a very active area of research. Recently, Oxone, as a new gentle, green and efficient oxidant shows great efficiency in many oxidative transformations, has received sustainable attention. This article will expand the relevant research work along this line of thought. In this paper, the synthesis methods of2-substituted benzoxazinones have been briefly reviewed. Then, the oxidation of2-substituted indoles to obtain2-substituted benzoxazinones in the oxidation of oxone has been achieved by control of oxidants and solvent under mild reaction conditions.