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Synfacts 2010(4): 0378-0378  
DOI: 10.1055/s-0029-1219488
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of SB-406725A

Contributor(s): Philip Kocienski
M. D. Walker*, B. I. Andrews, A. J. Burton, L. D. Humphreys, G. Kelly, M. B. Schilling, P. W. Scott
GlaxoSmithKline Pharmaceuticals, Stevenage, UK
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Publikationsdatum:
22. März 2010 (online)

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Significance

SB-406725A is an anticonvulsant lead for the treatment of epilepsy, migraine, and neuropathic pain. Major challenges in the large-scale synthesis of SB-406725A centered on the nitration of isoquinoline C and the selective reduction of the nitro group and the heterocyclic ring in D without simultaneous dechlorination.