反应详情

60 mg of DMAP, 130 mg of DIEA and 192 mg of EDC are added to a solution of 155 mg of 4-bromo-2,5-dichloro-thiophene-3-sulfonamide and 230 mg of 1-(tert.butyloxycarbonyl)-piperidine-4-carboxylic acid in 8 ml of DMF. The mixture obtained is stirred for ca. 16 h at ca. 30°, solvent is evaporated and the evaporation residue is treated with EtAc. The mixture obtained is washed with aqueous 1 N HCl, aqueous saturated NaHCO3 and brine, and dried. Solvent from the organic phase obtained is evaporated and the evaporation residue is subjected to chromatography. 4-(4-Bromo-2,5-dichloro-thiophene-3-sulfonylaminocarbonyl)-piperidine-1-carboxylic acid tert.-butyl ester is obtained and lyophilized from 1,4-dioxane.

1. customThe mixture obtained
2. customsolvent is evaporated
3. additionthe evaporation residue is treated with EtAc
4. customThe mixture obtained
5. washis washed with aqueous 1 N HCl, aqueous saturated NaHCO3 and brine
6. customdried
7. customSolvent from the organic phase obtained
8. customis evaporated