1-(2-Methoxymethoxyphenyl)-5,5-dimethylpiperazin-2-one → N-{(S)-1-[(2S,4S)-4-isopropyl-5-oxotetrahydrofuran-2-yl]-2-[4-(2-methoxymethoxyphenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]ethyl}-2-nitrobenzenesulfonamide

Participants

Reaction Steps

A solution of 214 mg of (3S,5S)-3-isopropyl-5-[(S)-1-(2-nitrobenzenesulfonyl)aziridin-2-yl]dihydrofuran-2-one obtained in Example (1g) (0.60 mmol) and 207 mg of 1-(2-methoxymethoxyphenyl)-5,5-dimethylpiperazin-2-one obtained in Example (12a) (0.78 mmol) in toluene (7 ml) was stirred at 110° C. for 45 minutes. After cooling, the reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (elution solvent:methylene chloride/methanol=20/1) to obtain 326 mg of N-{(S)-1-[(2S,4S)-4-isopropyl-5-oxotetrahydrofuran-2-yl]-2-[4-(2-methoxymethoxyphenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]ethyl}-2-nitrobenzenesulfonamide (yield: 87%).

Provenance & Evidence