Development of Large-Scale Routes to Potent GPR119 Receptor Agonists

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• 作者：Richard T. Matsuoka ; Eric E. Boros ; Andrew D. Brown ; Kae M. Bullock ; Will L. Canoy ; Andrew J. Carpenter ; Jeremy D. Cobb ; Shannon E. Condon ; Nicole M. Deschamps ; Vassil I. Elitzin ; Greg Erickson ; Jing M. Fang ; David H. Igo ; Biren K. Joshi ; Istvan W. Kaldor ; Mark B. Mitchell ; Gregory E. Peckham ; Daniel W. Reynolds ; Matthew C. Salmon ; Matthew J. Sharp ; Elie A. Tabet ; Jennifer F. Toczko ; Lianming Michael Wu ; Xiao-ming M. Zhou
• 刊名：Organic Process Research & Development
• 出版年：2016
• 出版时间：August 19, 2016
• 年：2016
• 卷：20
• 期：8
• 页码：1469-1475
• 全文大小：323K
• 年卷期：0
• ISSN：1520-586X

文摘

Practical and scalable syntheses were developed that were used to prepare multikilogram batches of GSK1292263A (<b>1b>) and GSK2041706A (<b>15b>), 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 Sb>Nb>Ar synthetic strategy.