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PubMed · 4639761

[Protease inhibitors].

P Metais·J Bieth

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P Metais, J Bieth. 1972. [Protease inhibitors].. https://pubmed.ncbi.nlm.nih.gov/4639761/

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A concise synthesis of silanediol-based transition-state isostere inhibitors of proteases.

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

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