Parallel synthesis of isatin-based serine protease inhibitors

Author:

Shuttleworth Stephen J.,Nasturica Daniel,Gervais Christian,Siddiqui M.Arshad,Rando Robert F.,Lee Nola

Publisher

Elsevier BV

Subject

Organic Chemistry,Clinical Biochemistry,Drug Discovery,Pharmaceutical Science,Molecular Biology,Molecular Medicine,Biochemistry

Reference23 articles.

1. N-(carbobenzyloxy)isatin: A slow binding α-keto lactam inhibitor of α-chymotrypsin

2. Design, Synthesis, and Evaluation of Nonpeptidic Inhibitors of Human Rhinovirus 3C Protease

3. Available from Fluka.

4. Aminomethyl polystyrene resin (1.0 equiv, 1.2mmol/g loading) from Novabiochem, or preferably a pre-packed cartridge containing an amine sorbent [bonded silica (aminopropyl functionality) of 0.6meq/g capacity] from IST Technologies Ltd were both used effectively. Isolation of products in parallel was accomplished using a 20 channel vacuum manifold available from IST Technologies Ltd.

5. Polymer supported bases in solution-phase synthesis. 2. A convenient method for N-alkylation reactions of weakly acidic heterocycles

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