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Ligand‐Promoted C(sp3)−H Olefination en Route to Multi‐functionalized Pyrazoles |
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| Authors: | Dr. Weibo Yang Dr. Shengqing Ye Yvonne Schmidt Dean Stamos Prof. Dr. Jin‐Quan Yu |
| Affiliation: | 1. Department of Chemistry, The Scripps Research Institute (TSRI), La Jolla, CA, USA;2. Medicinal Chemistry, Vertex Pharmaceuticals, San Diego, CA, USA |
| Abstract: | A Pd‐catalyzed/N‐heterocycle‐directed C(sp3)?H olefination has been developed. The monoprotected amino acid ligand (MPAA) is found to significantly promote Pd‐catalyzed C(sp3)?H olefination for the first time. Cu(OAc)2 instead of Ag+ salts are used as the terminal oxidant. This reaction provides a useful method for the synthesis of alkylated pyrazoles. |
| Keywords: | amino acid ligands C− H activation olefination organic chemistry pyrazole |