反应详情

To a solution of cis-4-(2-amino-6-(4-methoxybenzyloxy)-1H-benzo[d]imidazol-1-yl)-N-isopropylcyclohexanecarboxamide (424 mg, 0.971 mmol) and 4-fluorobenzoyl chloride (0.172 mL, 1.457 mmol) in DCM was added TEA (0.271 mL, 1.943 mmol), and the resulting mixture was stirred at RT for 10 minutes. The mixture was evaporated, and the residue diluted with DCM, washed with water, brine, and the organic layer dried over Na2SO4. The mixture was purified via flash chromatography using a linear gradient of 0% to 10% MeOH in DCM. The title compound was obtained as a tan foam (442 mg, max 80% yield, mixture of the mono and bis-acylated products).

1. customThe mixture was evaporated
2. additionthe residue diluted with DCM
3. washwashed with water, brine
4. dry with materialthe organic layer dried over Na2SO4
5. customThe mixture was purified via flash chromatography