反应详情

To mixture of 5-chloro-2-(3-(3-fluorophenoxy)azetidin-1-yl)nicotinic acid (D77) (60 mg, 0.186 mmol) in dry dimethylformamide (1 ml), 1-Hydroxybenzotriazole hydrate (28.5 mg, 0.189 mmol), 1-Ethyl-3-[3-dimethylaminopropyl]carbodiimide Hydrochloride (53.5 mg, 0.279 mmol) were added followed by the addition of a solution of 1-(4-(1H-tetrazol-5-yl)phenyl)cyclopropanamine hydrochloride (D17) (44.2 mg, 0.186 mmol) and triethylamine (26 μl, 0.189 mmol) in dry dimethylformamide. The mixture was stirred for 1 h at room temperature. The solvent was evaporated in vacuo and the resulting residue was taken in NH4Cl sat. sol (10 ml) and extracted with ethylacetate (2×10 ml). Collected organics after solvent evaporation afforded a residue that was washed with methanol (2 ml) to afford the title compound (E82) (30.8 mg)

1. additionwere added
2. customThe solvent was evaporated in vacuo
3. extractionextracted with ethylacetate (2×10 ml)
4. customCollected organics after solvent evaporation
5. customafforded a residue that
6. washwas washed with methanol (2 ml)