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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container_end_page 1475
container_issue 8
container_start_page 1469
container_title Organic process research & development
container_volume 20
creator 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
description 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.
doi_str_mv 10.1021/acs.oprd.6b00157
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title Development of Large-Scale Routes to Potent GPR119 Receptor Agonists
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