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Microwave-assisted four-component reaction for the synthesis of a monothiohydantoin inhibitor of a fatty acid amide hydrolase |
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| Authors: | Estelle Gallienne Didier M Lambert Michael Shipman |
| Institution: | a Department of Chemistry, University of Warwick, Gibbet Hill Road, Coventry CV4 7AL, UK b Unité de Chimie pharmaceutique et de Radiopharmacie, Ecole de Pharmacie, Faculté de Médecine, UCL, Avenue E. Mounier 73, UCL-CMFA 7340, B-1200 Brussels, Belgium c Drug Design and Discovery Center, FUNDP, rue de Bruxelles 61,B-5000 Namur, Belgium |
| Abstract: | Monothiohydantoin 3a is made in seven steps from 1,4-diiodobenzene and is shown to be an inhibitor of fatty acid amide hydrolase (IC50 = 23.4 ± 1.1 μM). The key step in the sequence involves a microwave-assisted four-component reaction that makes the 5,5′-disubstituted hydantoin nucleus by the sequential formation of two C-C and two C-N bonds. |
| Keywords: | FAAH Thiohydantoins Bucherer-Bergs reaction Multi-component reactions Microwaves |
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