Synthesis of Oxazolo[4,5-c]quinoline TRPV1 Antagonists

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• 作者：Eric A. Voight ; Jerome F. Daanen ; Michael E. Kort
• 刊名：Journal of Organic Chemistry
• 出版年：2010
• 出版时间：December 17, 2010
• 年：2010
• 卷：75
• 期：24
• 页码：8713-8715
• 全文大小：727K
• 年卷期：v.75,no.24(December 17, 2010)
• ISSN：1520-6904

文摘

An efficient synthesis of 2-amino-oxazolo[4,5-c]quinoline TRPV1 antagonists is described via a thiourea formation/carbodiimide cyclization sequence. Synthetic route optimization eliminates intermediate isolations and facilitates the rapid preparation of a series of novel pentacyclic TRPV1 antagonists. From this series, compound (S)-4 was identified as a potent and selective ligand for the TRPV1 ion channel.