Development of Large-Scale Routes to Potent GPR119 Receptor Agonists

Practical and scalable syntheses were developed that were used to prepare multikilogram batches of GSK1292263A (1) and GSK2041706A (15), two potent G protein-coupled receptor 119 (GPR119) agonists. Both syntheses employed relatively cheap and readily available starting materials, and both took advan...

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Veröffentlicht in:Organic process research & development 2016-08, Vol.20 (8), p.1469-1475
Hauptverfasser: Matsuoka, Richard T, Boros, Eric E, Brown, Andrew D, Bullock, Kae M, Canoy, Will L, Carpenter, Andrew J, Cobb, Jeremy D, Condon, Shannon E, Deschamps, Nicole M, Elitzin, Vassil I, Erickson, Greg, Fang, Jing M, Igo, David H, Joshi, Biren K, Kaldor, Istvan W, Mitchell, Mark B, Peckham, Gregory E, Reynolds, Daniel W, Salmon, Matthew C, Sharp, Matthew J, Tabet, Elie A, Toczko, Jennifer F, Wu, Lianming Michael, Zhou, Xiao-ming M
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Sprache:eng
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Zusammenfassung:Practical and scalable syntheses were developed that were used to prepare multikilogram batches of GSK1292263A (1) and GSK2041706A (15), two potent G protein-coupled receptor 119 (GPR119) agonists. Both syntheses employed relatively cheap and readily available starting materials, and both took advantage of an SNAr synthetic strategy.
ISSN:1083-6160
1520-586X
DOI:10.1021/acs.oprd.6b00157