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Rapid catalyst identification for the synthesis of the pyrimidinone core of HIV integrase inhibitors |
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| Authors: | Bellomo Ana Celebi-Olcum Nihan Bu Xiaodong Rivera Nelo Ruck Rebecca T Welch Christopher J Houk Kendall N Dreher Spencer D |
| Affiliation: | Department of Chemistry, University of Pennsylvania, Philadelphia, 19104-6323, USA. |
| 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. |
| Keywords: | heterocycles high‐throughput screening homogeneous catalysis P ligands synthetic methods |
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