The Carbon-Nitrogen bond formation has always been an important and useful tool in drug discovery. Its wide applications in synthesizing N-heterocycles, known as the most prevalent moiety in the active pharmacophores, have attracted increasing attention from researchers. In recent years many works were devoted to finding new and more rapid and effective chemo-and regio-selective methods for the synthesis of N-containing heterocycles. Buchwald-Hartwig and Ullman-Goldberg are two proven efficient methods for synthesizing five, six, and seven-membered heterocycles found abundantly in literature. Here, we study these two amination methods more precisely, based on the reaction conditions and the products.

Coumarin is an important pharmaceutical structural motif, abundantly found in numerous commonly used drugs. Compounds containing this core show a broad spectrum of medicinal properties and biological activities. The increasing...

A highly efficient and practical procedure for chemoand regioselective synthesis of ortho-diacylbenzenes through Pd-catalyzed oxidative C-H bond activation has been developed. Using this method, a variety of ortho-diacylbenzenes