Ullmann-Goldberg and Buchwald-Hartwig C-N Cross Couplings: Synthetic Methods to Pharmaceutically Potential N-Heterocycles

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.

Automated summary

Carbon-nitrogen bond formation is a crucial tool in drug discovery, with Buchwald-Hartwig and Ullman-Goldberg methods being proven efficient for synthesizing heterocycles. Researchers have been focusing on developing new and faster methods for N-containing heterocycle synthesis.