Organic Process Research & Development · 2016 · 10 citations · 3 references
Medicinal ChemistryMultikilogram BatchesBiochemistryFunctional SelectivityMedicineNatural SciencesG Protein-coupled ReceptorGlycobiologyReceptor (Biochemistry)Large-scale RoutesPeptide SynthesisPharmacotherapySnar Synthetic StrategyPharmacologyScalable SynthesesDrug DiscoveryGlycosylation
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.
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