反应详情

To [4-(4-methoxy-benzoyl)-piperidin-1-yl]-acetic acid (306 mg, 0.85 mmol) in DMF (3 mL) was added with HATU (485 mg, 1.28 mmol) and DIEA (0.37 mL, 275 mg, 2.12 mmol). This was sonicated, stirred for 30 min and then 2-[(cyclopropylmethyl-amino)-methyl]-3,5,7,8-tetrahydro-pyrano[4,3-d]pyrimidin-4-one (200 mg, 0.85 mmol) in 1 mL DMF was added to the mixture. Then it was stirred at room temperature for 16 hours and the mixture was concentrated to dryness. This was purified by silica gel column (eluted with 0-10% methanol in dichloromethane) followed by trituration with methanol to give a white solid as the title compound (93 mg, 0.19 mmol, 22% yield). m/z=495.3 (M+H).

1. customThis was sonicated
2. stirringThen it was stirred at room temperature for 16 hours
3. concentrationthe mixture was concentrated to dryness
4. customThis was purified by silica gel column (eluted with 0-10% methanol in dichloromethane)