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Synfacts 2006(12): 1205-1205  
DOI: 10.1055/s-2006-955596
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of Lu AA20465

Contributor(s): Philip Kocienski
E. A. Krafft, E. Pinard, A. W. Thomas*
Hofmann-La Roche LTD., Basel, Switzerland
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Publication History

Publication Date:
22 November 2006 (online)

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Significance

Lu AA20465 inhibits GlyT1, a transporter co-expressed in the brain along with NMDA, which selectively uptakes glycine into neuronal cells. It is under development for the treatment of schizophrenia. The synthesis depicted is an improvement of a known route (G. Smith et al. Bioorg. Med. Chem. Lett. 2004, 14, 4027-4030). Salient features are (a) a diazotization-iodination under anhydrous conditions and (b) a Cu(I)-catalyzed S-arylation.