反应详情

A solution of 2-bromo-thiazole-4-carboxylic acid (Intermediate 3; 21.2 mmol), decahydroquinoline (3.54 g, 25.4 mmol), DIPEA (7.4 mL, 42.4 mmol), and PyBrop (11.9 g, 25.4 mmol) in dry DCM (70 mL) was stirred overnight at room temperature. The mixture was extracted with DCM and water three times. The combined DCM extracts were evaporated, and the residue was chromatographed on silica, eluting with EtOAc/Hexane (0-10% gradient) to give (2-bromo-thiazol-4-yl)-(octahydro-quinolin-1-yl)-methanone (6.0 g, 86%).

1. extractionThe mixture was extracted with DCM and water three times
2. customThe combined DCM extracts were evaporated
3. customthe residue was chromatographed on silica
4. washeluting with EtOAc/Hexane (0-10% gradient)