Rapid catalyst identification for the synthesis of the pyrimidinone core of HIV integrase inhibitors

Abstract

A microscale chemistry improvement engine: A pre-dosed microscale high-throughput experimentation additives platform enables rapid, serendipitous reaction improvement. This platform allowed one chemist to set up 475 experiments and analyze the results using MISER chromatography in a single day, thus resulting in two high-quality catalytic systems for the construction of the title compound 1. Support for a single-electron transfer mechanism was obtained. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.