Polymer-supported reagents and scavengers to streamline tedious purification steps

Yadav-Bhatanagar, N.; Desjonque`res, N.; Mauger, J. Polymer-Supported Approach for Solution-Phase Synthesis of Cysteine Trap Protease Inhibitors: Procedure for Straightforward Optimization of the P1-P1' Pocket. J. Comb. Chem 2002, 4, 49-55.

Peptide-based reversible and irreversible cysteine proteases inhibitors are well reported in the literature.  Many of these compounds have an electrophilic carbonyl group as a cysteine trap in the place of a scissile amide moiety of the natural substrate. As a common mechanism strategy, we have designed a probe library of a cysteine trap for rapid optimization of P1-P1¢ pockets of different cysteine proteases. The synthesis of this library using a straightforward methodology based on polymer-supported reagents and scavengers to avoid tedious purification steps has been achieved. For the selective monobromination of diazo ketones, preparation of a new supported reagent, piperidinoaminomethylpolystyrene hydrobromide, is also described.

Polymer-Supported Approach for Solution-Phase Synthesis of Cysteine Trap Protease Inhibitors: Procedure for Straightforward Optimization of the P1-P1'Pocket

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Applications

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• Solution Phase Synthesis Using a MiniBlock
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