反应详情

To a stirred solution of 5.80 g (15.6 mmol) 1-benzoyl-3-(5-methoxy-2-morpholin-4-yl-pyridin-4-yl)-thiourea in 100 ml tetrahydrofuran and 25 ml methanol heated at 60° C. was added dropwise 1.15 ml (6.23 mmol) 5.4 M sodium methylate solution and stirring continued for 2 h at 60° C. 1.2 ml concentrated hydrochloric acid was then added and the reaction mixture concentrated in vacuo. The residue was triturated in 25 ml ether to afford 3.51 g (84%) (5-methoxy-2-morpholin-4-yl-pyridin-4-yl)-thiourea as alight brown crystalline solid. ES-MS m/e (%): 269 (M+H+, 100).

1. concentrationthe reaction mixture concentrated in vacuo
2. customThe residue was triturated in 25 ml ether