Reacción #169679

Ecuación de reacción

niacin

N-methyl morpholine

L-leucinemethyl ester hydrochloride

→

required product

Rendimiento 72.6%

4-methyl-2-[pyridine-3-carbonyl]-amino-pentanoic acid methyl ester

Rendimiento 72.6%

Disolventes

DCM

DCM

Condiciones de reacción

Tratamiento posterior

1. 1
   Lavadowashed with water (3×100 mL)
2. 2
   Secadodried over sodium sulphate
3. 3
   OtroThe crude product obtained upon evaporation of the solvent
4. 4
   Otrowas further purified by silica gel column chromatography

Procedimiento

To a solution of niacin (1.35 g, 11.0 mmol) in DCM (20 mL) were added N-methyl morpholine (3.34 g, 33.00 mmol) EDCI.HCl (4.2 g, 22.02 mmol), and L-leucinemethyl ester hydrochloride (2.0 g, 11.0 mmol). The mixture was allowed to stir at room temperature (25° C.) over 2.5 h under nitrogen atmosphere. The resulting mixture was diluted with DCM (200 mL), washed with water (3×100 mL) and dried over sodium sulphate. The crude product obtained upon evaporation of the solvent was further purified by silica gel column chromatography to obtain required product as white solid (2.0 g, 72%).

Fuente