반응 #61716

반응 방정식

(3S)-3-amino-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]pyrrolidin-2-one

Intermediate 40

(3S)-3-amino-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]pyrrolidin-2-one

5-chloro-1-benzofuran-2-sulfonyl chloride

Intermediate 51

5-chloro-1-benzofuran-2-sulfonyl chloride

ammonium chloride

→

title compound

수율 55.1%

5-Chloro-N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}-1-benzofuran-2-sulfonamide

수율 55.1%

용매

acetonitrile

acetonitrile

pyridine

반응 조건

후처리

1. 1
   농축The mixture was concentrated under reduced pressure
2. 2
   기타the residue partitioned between chloroform and hydrochloric acid (2M)
3. 3
   세척The organic layer was washed with saturated sodium bicarbonate and brine
4. 4
   기타The organic layer was isolated
5. 5
   건조dried (over magnesium sulphate)
6. 6
   농축concentrated under reduced pressure

실험 절차

To a solution of (3S)-3-amino-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]pyrrolidin-2-one [Intermediate 40] (0.077 g) in anhydrous acetonitrile (2 ml) were added 5-chloro-1-benzofuran-2-sulfonyl chloride [Intermediate 51] (0.043 g) in acetonitrile (2 ml) and pyridine (0.057 ml), and the mixture was stirred at room temperature for 72 h. Saturated ammonium chloride solution (2 ml) was added and the resultant mixture stirred at room temperature for 20 min. The mixture was concentrated under reduced pressure and the residue partitioned between chloroform and hydrochloric acid (2M). The organic layer was washed with saturated sodium bicarbonate and brine. The organic layer was isolated, dried (over magnesium sulphate) and concentrated under reduced pressure to give the title compound (0.043 g) as a white solid.

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