Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 22, Issue 21, Pages 7059-7062Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201600704
Keywords
amino acid ligands; C-H activation; olefination; organic chemistry; pyrazole
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Funding
- Scripps Research Institute
- Vertex Pharmaceuticals, Inc
- NIH (NIGMS) [5R01 GM102265]
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A Pd-catalyzed/N-heterocycle-directed C(sp(3))-H olefination has been developed. The monoprotected amino acid ligand (MPAA) is found to significantly promote Pd-catalyzed C(sp(3))-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.
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