Triethylamine → 7-(2-furyl)-N-(4-((N-tetrahydropyran-4-yl-N-methylamino)methyl)-phenyl)-2,3-dihydro-1-benzoxepine-4-carboxamide

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Reaction Steps

To a solution of 7-(2-furyl)-2,3-dihydro-1-benzoxepine-4-carboxylic acid (0.15g), 4-(N-methyl-N-(tetrahydropyran-4-yl)aminomethyl)aniline (0.15g) and triethylamine (0.25ml) in dimethylformamide (10ml) was added diethyl cyanophosphate (0.13ml) under ice-cooling, and the mixture was stirred under nitrogen atmosphere at room temperature over night. The solvent was evaporated, and the residue was purified with silica gel column (methanol/ethyl acetate/triethylamine) to give crude crystals, which were recrystallized from ethyl acetate-hexane to give 7-(2-furyl)-N-(4-((N-tetrahydropyran-4-yl-N-methylamino)methyl)-phenyl)-2,3-dihydro-1-benzoxepine-4-carboxamide (Compound 148) (0.1g) as brown crystals.

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