Microwave-Enhanced α-Arylation of a Protected Glycine in Water:Evaluation of 3-Phenylglycine Derivatives as Inhibitors of the Tuberculosis Enzyme, Glutamine Synthetase

Title: Microwave-Enhanced α-Arylation of a Protected Glycine in Water:Evaluation of 3-Phenylglycine Derivatives as Inhibitors of the Tuberculosis Enzyme, Glutamine Synthetase

Volume: 10 Issue: 9

Author(s): Olof Lagerlund, Luke R. Odell, Sherry L. Mowbray, Mikael T. Nilsson, Wojciech W. Krajewski, Anneli Nordqvist, Anders Karlen and Mats Larhed

Affiliation:

Keywords: Arylation, glutamine synthetase, microwave, palladium, tuberculosis, water

Abstract: A microwave-enhanced, palladium-catalyzed protocol for the α-arylation of a protected glycine in neat water is described. This reaction proceeds rapidly, under non-inert conditions, to afford a range of phenylglycine derivatives in moderate to good yields. Based on this α-arylation, a number of aryl L-methionine-SR-sulfoximine (MSO) analogues were prepared and evaluated for their Mycobacterium tuberculosis glutamine synthetase (TB-GS) inhibitory activity.

Cite this article as:

Lagerlund Olof, Odell R. Luke, Mowbray L. Sherry, Nilsson T. Mikael, Krajewski W. Wojciech, Nordqvist Anneli, Karlen Anders and Larhed Mats, Microwave-Enhanced α-Arylation of a Protected Glycine in Water:Evaluation of 3-Phenylglycine Derivatives as Inhibitors of the Tuberculosis Enzyme, Glutamine Synthetase, Combinatorial Chemistry & High Throughput Screening 2007; 10 (9) . https://dx.doi.org/10.2174/138620707783018478