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

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• 作者：Eric A. Voight ; Jerome F. Daanen ; Robert G. Schmidt ; Arthur Gomtsyan ; Michael J. Dart ; Philip R. Kym
• 刊名：Journal of Organic Chemistry
• 出版年：2016
• 出版时间：December 2, 2016
• 年：2016
• 卷：81
• 期：23
• 页码：12060-12064
• 全文大小：328K
• ISSN：1520-6904

文摘

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.