Synthesis of Glycine Transporter Inhibitor GSK2137305

J. P. Graham; N. Langlade; J. M. Northall; A. J. Roberts; A. J. Whitehead

doi:10.1055/s-0030-1259590

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Synfacts 2011(4): 0354-0354
DOI: 10.1055/s-0030-1259590

Synthesis of Natural Products and Potential Drugs

Synthesis of Glycine Transporter Inhibitor GSK2137305

Contributor(s): Philip Kocienski
J. P. Graham*, N. Langlade, J. M. Northall, A. J. Roberts, A. J. Whitehead
GlaxoSmithKline, Stevenage, UK

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Publication History

Publication Date:
18 March 2011 (online)

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Significance

GSK2137305 is a glycine transporter type-1 (GlyT1) inhibitor with potential for the treatment of neurological and neuropsychiatric disorders. The principle challenge in the synthesis depicted was the construction of the spirocyclic imidazoldinone D from the α-amino nitrile B generated in situ by a Strecker reaction.