反应详情

温度

40 °C

A mixture of 1-[(3,4-dichlorophenyl)methyl]-1H-1,2,3-triazole-4-carboxylic acid (Intermediate 11) (1 g, 3.6 mmol), methyl 2-amino-1,3-thiazole-5-carboxylate (0.58 g, 3.6 mmol), HATU (1.82 g, 1.3 eq) and DIPEA (0.9 mL, 1.3 eq) in DMF (50 mL) was stirred at 40° C. for 3 days. The solvent was evaporated and the residue was washed with water and extracted with DCM. A precipitate was formed, filtered and triturated with a mixture of methanol/acetonitrile. After filtration, the yellow solid was dried to give the title compound as a pale yellow solid (644 mg, 44%). LC/MS: m/z 412 (M+H)+. Rt: 3.21 min.

1. customThe solvent was evaporated
2. washthe residue was washed with water
3. extractionextracted with DCM
4. customA precipitate was formed
5. filtrationfiltered
6. customtriturated with a mixture of methanol/acetonitrile
7. filtrationAfter filtration
8. customthe yellow solid was dried