Solid-phase synthesis of isoquinolinones using Bischler-Napieralski cyclization

A traceless solid-phase synthetic approach to isoquinolinones is described here. This approach allows introducing both electron-donating as well as electron-withdrawing moieties on the benzene nuclei of isoquinolinones with high yields and purities. Isoquinolinone is a structural unit found in many natural products having various important biological activities. A traceless solid-phase synthetic approach has been developed to prepare isoquinolinone derivatives. This approach enables one to synthesize isoquinolinones having various moieties on benzene nuclei and also can produce derivatives with a proton on the amide nitrogen.