反应详情

1.69 g of 3-mercaptopyridine-2-carboxylic acid were dissolved in 20 ml of DMF and 7.5 ml of N-ethylmorpholine, 1.7 g of 1-hydroxy-1H-benzotriazole, 5 g of N-cyclohexyl-N'-(2-morpholinoethyl)-carbodiimide methyl-p-toluenesulfonate and 4.3 g of glycine methyl ester hydrochloride were added successively at room temperature and whilst stirring. After having been stirred for 12 hours, the mixture was partitioned between a saturated aqueous solution of ammonium chloride and dichloromethane and the organic phase was dried and concentrated by evaporation; the residue was purified by chromatography on silica gel (eluent: ethyl acetate/heptane); yield, 0.65 g of colourless crystals of m.p. 178°-179° C. (ethyl acetate/heptane).

1. stirringAfter having been stirred for 12 hours
2. customthe mixture was partitioned between a saturated aqueous solution of ammonium chloride and dichloromethane
3. customthe organic phase was dried
4. concentrationconcentrated by evaporation
5. customthe residue was purified by chromatography on silica gel (eluent: ethyl acetate/heptane)
6. customyield