Reacción #219761

Ecuación de reacción

HATU

acetonitrile

1-{1-[3-(2-aminophenoxy)-2-hydroxy-2-methylpropyl]-4-piperidinyl}-1,3-dihydro-2H-benzimidazol-2-one

2-pyridinecarboxylic acid

Hünigs base

→

N-(2-{2-Hydroxy-2-methyl-3-[4-(2-oxo-2,3-dihydro-1H-benzimidazol-1-yl)-1-piperidinyl]propoxy}phenyl)-2-pyridinecarboxamide

Disolventes

THF

Condiciones de reacción

Tratamiento posterior

1. 1
   Concentración2 h at room temperature the reaction mixture was concentrated
2. 2
   Otrothe residue purified on silica (dichloromethane-methanol, 12:1, containing 1% of NH4OH (25%))

Procedimiento

HATU in acetonitrile (0.2 M, 0.375 ml, 0.075 mmol) was added to a solution of 1-{1-[3-(2-aminophenoxy)-2-hydroxy-2-methylpropyl]-4-piperidinyl}-1,3-dihydro-2H-benzimidazol-2-one (0.020 g, 0.05 mmol), 2-pyridinecarboxylic acid (0.006 g, 0.05 mmol) and Hünigs base (0.013 ml, 0.075 mmol) in THF (0.5 ml). After 0.5 h at 40° C. and 2 h at room temperature the reaction mixture was concentrated, and the residue purified on silica (dichloromethane-methanol, 12:1, containing 1% of NH4OH (25%)). Yield 20 mg of the title compound.

Fuente