A Concise Synthesis of Silanediol-Based Transition-State Isostere Inhibitors of Proteases

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• 作者：Michael G. Organ ; Christophe Buon ; Carl P. Decicco ; and Andrew P. Combs
• 刊名：Organic Letters
• 出版年：2002
• 出版时间：August 8, 2002
• 年：2002
• 卷：4
• 期：16
• 页码：2683 - 2685
• 全文大小：36K
• 年卷期：v.4,no.16(August 8, 2002)
• ISSN：1523-7052

文摘

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An efficient synthesis of silanediol-based transition-state inhibitors of proteases is described. A new convergent synthesis has been optimizedby using a two-step sequence of hydrosilylation followed by the addition of a silyllithio species to an imine. The method should be applicableto the synthesis of a wide variety of silanediol isosteres to probe the utility of this unique transition-state isostere.

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