5-AMINO-N-METHYLPYRIDINE-2-CARBOXAMIDE synthesis

Yield:-

Reaction Conditions:

with triethylamine;HATU in N,N-dimethyl-formamide at 20; for 16 h;

Steps:

5-Amino-pyridine-2-carboxylic acid (leq.), HATU (1.5 eq.) and Et₃N (2eq.) are mixed in DMF at room temperature, methylamine (l.leq.) is added to the solution and the reaction mixture is stirred at room temperature for 16hrs. Water is added to the reaction. The organic phases are isolated, dried over MgS O₄, filtered and evaporated under vacuum to afford the expected product. In same cases, purification by flash chromatography is required.

References:

GALAPAGOS NV;MENET, Christel Jeanne Marie;BLANC, Javier;JOUANNIGOT, Nolwenn;HODGES, Alastair James;VAN ROMPAEY, Luc Juliaan Corina;FLETCHER, Stephen Robert WO2010/10189, 2010, A1 Location in patent:Page/Page column 69