Optimisation of Permanganate Oxidation and Suzuki− Miyaura Coupling Steps in the Synthesis of a Nav1. 8 Sodium Channel Modulator
…, AT Gillmore, MS Glossop, DJ McManus…
文献索引:Fray, M. Jonathan; Gillmore, Adam T.; Glossop, Melanie S.; McManus, David J.; Moses, Ian B.; Praquin, Celine F.B.; Reeves, Keith A.; Thompson, Lisa R. Organic Process Research and Development, 2010 , vol. 14, # 1 p. 263 - 271
The development is described of a viable kilo-scale synthesis of the Nav1. 8 sodium channel modulator, N-methyl-6-amino-5-(2, 3, 5-trichlorophenyl) pyridine-2-carboxamide (PF- 1247324) in five steps, starting from 6-amino-5-bromo-2-picoline, in 33% overall yield. ...