تفاعل #61717

معادلة التفاعل

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

المذيبات

water

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةThe mixture was then heated at 80° C. for 8 h
2. 2
   درجة الحرارةcooled
3. 3
   استخلاصThe organic extract
4. 4
   تجفيفwas dried (over magnesium sulphate)
5. 5
   تركيزconcentrated under reduced pressure
6. 6
   أخرىThe residue was purified

الإجراء التجريبي

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.

المصدر