反应详情

0.8 ml (5.7 mmol) of triethylamine then 0.4 ml (5.7 mmol) of methanesulphonyl chloride are added to a solution of 2.2 g (3.6 mmol) of dimethyl 2-(4-tert-butoxycarbonylpiperazin-1-yl)-2-[(4-but-2-ynyloxybenzoylamino)methyl]malonate in 25 ml of dichloromethane. The reaction medium is then stirred at ambient temperature for 3 h, then the solvents are evaporated under vacuum and the crude product obtained is purified by chromatography over silica gel eluted with a 98/2 dichloromethane/methanol mixture. 2 g (80%) of dimethyl 2-[(4-but-2-ynyloxybenzoylamino)methyl]-2-(4-methane-sulphonylpiperazin-1-yl)malonate are obtained in the form of a white solid.

1. customthe solvents are evaporated under vacuum
2. customthe crude product obtained
3. customis purified by chromatography over silica gel
4. washeluted with a 98/2 dichloromethane/methanol mixture