Diisopropylethylamine → N-Cyclopropylmethyl-2-[4-(4-fluoro-benzoyl)-piperidin-1-yl]-N-(4-oxo-3,5,7,8-tetrahydro-4H-pyrano[4,3-d]pyrimidin-2-ylmethyl)-acetamide

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Reaction Steps

[4-(4-Fluoro-benzoyl)-piperidin-1-yl]-acetic acid (169 mg, 0.64 mmol) was added with HATU (364 mg, 0.96 mmol) in DMF (2 mL) and DIEA (0.28 mL, 1.60 mmol) was added. 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 (150 mg, 0.64 mmol) in 1 mL DMF was added to the mixture. The mixture was stirred at room temperature for 16 h, concentrated to dryness, purified by silica gel column (eluted with 0-10% methanol in dichloromethane) then triturated with methanol to give a white solid as the title compound (66 mg, 0.14 mmol, 21% yield). m/z=483.3 (M+H).

Provenance & Evidence