反应详情

1.00 g (4.0 mmol) of (2′,5′-difluoro[1,1′-biphenyl]-4-yl)acetic acid and 0.54 g (4.0 mmol) of 1-hydroxy-1H-benzotriazole hydrate are introduced into 15 ml of dimethylformamide at room temperature. 0.84 g (4.0 mmol) of 2-methylamino-4-methyl-1,3-thiazole-5-sulfonamide and 0.77 g (4.0 mmol) of N′-(3-dimethylaminopropyl)-N-ethylcarbodiimide hydrochloride are added, and the mixture is stirred at room temperature for 18 h. The dimethylformamide is substantially removed at 50° C. under high vacuum, and the residue is stirred 3 times with 50 ml of water each time, filtered off, stirred with 50 ml of isopropanol and again filtered off. Removal of the solvent in vacuo results in the compound of Example 87 in the form of a pale yellow-colored solid.

1. customThe dimethylformamide is substantially removed at 50° C. under high vacuum
2. stirringthe residue is stirred 3 times with 50 ml of water each time
3. filtrationfiltered off
4. stirringstirred with 50 ml of isopropanol
5. filtrationagain filtered off
6. customRemoval of the solvent in vacuo