Réaction #61717

Équation de réaction

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

Solvants

water

Conditions de réaction

Traitement

1. 1
   TempératureThe mixture was then heated at 80° C. for 8 h
2. 2
   Températurecooled
3. 3
   ExtractionThe organic extract
4. 4
   Séchagewas dried (over magnesium sulphate)
5. 5
   Concentrationconcentrated under reduced pressure
6. 6
   AutreThe residue was purified

Mode opératoire

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 extract 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.

Source