反应详情

To a solution of (2S,4R)-2-[2-(hydroxymethyl)thiazol-4-yl]-4-methanesulfonyloxy-1-(4-nitrobenzyloxycarbonyl)pyrrolidine (2.1 g) in acetonitrile (50 ml) was added chlorosulfonyl isocyanate (0.48 ml) at 0°-5° C. and the mixture was stirred at ambient temperature for 1 hour. Water (3 ml) was added to the solution at the same temperature and the mixture was stirred for 20 hours. After the solvent was removed, the residue was dissolved in ethyl acetate, and washed with water, saturated sodium bicarbonate and brine successively. The dried organic layer was evaporated to give (2S,4R)-2-[2-(carbamoyloxymethyl)thiazol-4-yl]-4-methanesulfonyloxy-1-(4-nitrobenzyloxycarbonyl)pyrrolidine (2.2 g).

1. stirringthe mixture was stirred for 20 hours
2. customAfter the solvent was removed
3. dissolutionthe residue was dissolved in ethyl acetate
4. washwashed with water, saturated sodium bicarbonate and brine successively
5. customThe dried organic layer was evaporated