反应详情

To a solution of 2-(4-fluoro-benzyl)-malonic acid monomethyl ester, 56, (47.5 mg, 0.21 mmol), 4-cyclohexyl-4-[1,2,4]triazol-1-ylmethyl-piperidine, 18, (50 mg, 0.20 mmol), 1-hydroxybenzotriazole (54 mg, 0.40 mmol), 4-methylmorpholine (88 □l, 0.80 mmol) in N,N-dimethylformamide (7 mL) is added 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (50 mg, 0.26 mmol). The reaction mixture is stirred overnight and then aqueous ammonium chloride is added. The reaction is extracted with ethyl acetate, and the organics are separated dried over sodium sulfate, filtered and concentrated under reduced pressure. The crude product is purified by preparative HPLC to afford the desired compound.

1. extractionThe reaction is extracted with ethyl acetate
2. customthe organics are separated
3. dry with materialdried over sodium sulfate
4. filtrationfiltered
5. concentrationconcentrated under reduced pressure
6. customThe crude product is purified by preparative HPLC