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Combinatorial Chemistry & High Throughput Screening


ISSN (Print): 1386-2073
ISSN (Online): 1875-5402

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

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

Volume 10 , Issue 9 , 2007

Page: [783 - 789] Pages: 7

DOI: 10.2174/138620707783018478

Price: $65


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.

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

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