Total Synthesis of Leupyrrin B1: A Potent Inhibitor of Human Leukocyte Elastase

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• 作者：Sebastian Thiede ; Paul R. Wosniok ; Daniel Herkommer ; Anna-Christina Schulz-Fincke ; Michael Gütschow ; Dirk Menche
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：August 19, 2016
• 年：2016
• 卷：18
• 期：16
• 页码：3964-3967
• 全文大小：369K
• 年卷期：0
• ISSN：1523-7052

文摘

The total synthesis of leupyrrin B₁ was accomplished by an expedient strategy that involves an optimized HATU-mediated amide coupling protocol of elaborate substrates. The generally useful procedure was also successfully applied in an improved total synthesis of leupyrrin A₁. Finally, leupyrrins A₁ and B₁ were evaluated toward a panel of proteases, and human leukocyte elastase was discovered as a molecular target of the leupyrrins.