Reacción #7420

Ecuación de reacción

Example 1

tert-Butyl(2R)-2-((3R)-3-{[(6-chloro-2-naphthyl)sulfonyl]amino}-2-oxopyrrolidin-1-yl)propanoate

chloroethylmorpholine hydrochloride

potassium carbonate

ethyl acetate

DMF

→

title compound

6-Chloro-N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}-N-(2-morpholin-4-ylethyl)naphthalene-2-sulfonamide formate

Disolventes

water

Condiciones de reacción

Tratamiento posterior

1. 1
   TemperaturaThe mixture was then heated at 80° C. for 8 h
2. 2
   Temperaturacooled
3. 3
   SecadoThe organic extraxt was dried (over magnesium sulphate)
4. 4
   Concentraciónconcentrated under reduced pressure
5. 5
   OtroThe residue was purified

Procedimiento

Example 1 (0.05 g) was dissolved in DMF (1 ml) and treated with chloroethylmorpholine hydrochloride (0.062 g) and potassium carbonate (0.093 g), and stirred at 40° C. for 2 h. The mixture was then heated at 80° C. for 8 h, cooled and treated with ethyl acetate and water. The organic extraxt was dried (over magnesium sulphate) and concentrated under reduced pressure. The residue was purified using mass directed preparative h.p.l.c. to give the title compound (0.018 g) as a white solid.

Fuente