反应详情

(S)-2-(2-(difluoromethyl)-4-((2,2-dimethyl-1,3-dioxolan-4-yl)methoxy)phenyl)-1H-benzo[d]imidazole-4-carboxylic acid (67; 100 mg, 0.239 mmol) was taken up in 10 ml of DMF along with 2-aminothiazole (4; 28.7 mg, 0.289 mmol), HATU (181.7 mg, 0.478 mmol) and DIEA (61.8 mg, 0.289 mmol). The resulting reaction mixture was stirred at room temperature for 12 h and diluted with water. The precipitated solids were collected by filtration and dried. Purification by chromatography (EtOAc/Hexane=2:1) afforded (S)-2-(2-(difluoromethyl)-4-((2,2-dimethyl-1,3-dioxolan-4-yl)methoxy)phenyl)-N-(thiazol-2-yl)-1H-benzo[d]imidazole-4-carboxamide 68 (77 mg, 65%). MS (ESI) calcd for C24H22F2N4O4S: 500.13; found: 501 [M+H].

1. customThe resulting reaction mixture
2. filtrationThe precipitated solids were collected by filtration
3. customdried
4. customPurification by chromatography (EtOAc/Hexane=2:1)