反应详情

To a stirred solution of 0.330 g (1.4 mmol) 4-methoxy-N1-methyl-N1-(tetrahydro-pyran-4-ylmethyl)-benzene-1,3-diamine in 5 ml acetone was added dropwise 0.2 ml (1.50 mmol) benzoyl isothiocyanate and stirring continued for 16 hrs at room temperature. The mixture was then concentrated in vacuo and the residue subjected to column chromatography (1/1 hexane/ethyl acetate) to afford 0.31 g (56%) 1-benzoyl-3-{2-methoxy-5-[methyl-(tetrahydro-pyra n-4-yl)-amino]-phenyl}-thiourea as a yellow solid. ES-MS m/e (%): 422 (M+Na+, 13), 400 (M+H+, 100).

1. concentrationThe mixture was then concentrated in vacuo