反应详情

Combine 5-(3-aminomethyl-cyclohexyl)-3-methyl-5H-2-oxa-1,5,8-triaza-cyclopenta[a]naphthalen-4-one hydroiodide (145 mg, 0.33 mmol) with benzoic acid (44 mg, 0.36 mmol), 1-[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride (70 mg, 0.36 mmol), 1-hydroxy-7-azabenzo-triazole (49 mg, 0.36 mmol), and N,N-diisopropylethyl amine (0.20 mL, 1.15 mmol), in N,N-dimethylformamide (4 mL) and stir over the weekend at ambient temperature. Concentrate in vacuo and take up in water and extract with dichloromethane. Dry over sodium sulfate and concentrate in vacuo. Elute over silica gel using methanol/dichloromethane to give 98 mg (71%) of the desired product as a white solid. MS(ES): (M+1)+ 417.0, 418.1 m/z.

1. concentrationConcentrate in vacuo
2. extractionextract with dichloromethane
3. dry with materialDry over sodium sulfate
4. concentrationconcentrate in vacuo
5. washElute over silica gel