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

Ana Bellomo, Nihan Celebi-Olcum, Xiaodong Bu, Nelo Rivera, Rebecca T Ruck, Christopher J Welch, Kendall N Houk, Spencer D Dreher

Department of Chemistry, University of Pennsylvania, Philadelphia, 19104-6323, USA.

Angewandte Chemie (International ed. in English) 2012 Jul 9

filter terms:

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.

Citation

Ana Bellomo, Nihan Celebi-Olcum, Xiaodong Bu, Nelo Rivera, Rebecca T Ruck, Christopher J Welch, Kendall N Houk, Spencer D Dreher. Rapid catalyst identification for the synthesis of the pyrimidinone core of HIV integrase inhibitors. Angewandte Chemie (International ed. in English). 2012 Jul 9;51(28):6912-5