反应详情

At room temperature, 17.33 g (73.3 mmol) of (2′-fluoro[1,1′-biphenyl]4-yl)acetic acid and 9.9 g (73.3 mmol) of 1-hydroxy-1H-benzotriazole hydrate are initially charged in 600 ml of dimethylformamide. 16.84 g (81.4 mmol) of 2-methylamino-4-methyl-1,3-thiazole-5-sulphonamide and 15.58 g (81.4 mmol) of N′-(3-dimethylaminopropyl)-N-ethylcarbodiimide hydrochloride are added, and the mixture is stirred at room temperature for 18 h. Most of the dimethylformamide is removed at 50° C. under high vacuum, and the residue is taken up in 400 ml of dichloromethane and then washed with in each case 350 ml of water and 10% citric acid solution. Drying over magnesium sulphate and removal of the solvent under reduced pressure gives the compound of Example 57 in the form of a white solid.

1. customMost of the dimethylformamide is removed at 50° C. under high vacuum
2. washwashed with in each case 350 ml of water and 10% citric acid solution
3. dry with materialDrying over magnesium sulphate and removal of the solvent under reduced pressure