Stereoselective Synthesis of a Dipyridyl Transient Receptor Potential Vanilloid‑3 (TRPV3) Antagonist

An efficient asymmetric synthesis of dipyridyl TRPV3 antagonist 1 is reported. The four-step route involves two C–C bond-forming steps, a highly diastereoselective alkene hydration, and asymmetric ketone hydrosilylation in 97% ee.

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Veröffentlicht in:Journal of organic chemistry 2016-12, Vol.81 (23), p.12060-12064
Hauptverfasser: Voight, Eric A, Daanen, Jerome F, Schmidt, Robert G, Gomtsyan, Arthur, Dart, Michael J, Kym, Philip R
Format: Artikel
Sprache:eng
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Zusammenfassung:An efficient asymmetric synthesis of dipyridyl TRPV3 antagonist 1 is reported. The four-step route involves two C–C bond-forming steps, a highly diastereoselective alkene hydration, and asymmetric ketone hydrosilylation in 97% ee.
ISSN:0022-3263
1520-6904
DOI:10.1021/acs.joc.6b02443