反应详情

Step 1): To a solution of 5-fluoro-2-nitro-N-[(1-diphenylmethylpiperidin-4-yl)methyl]benzamide (2.0 g, 4.46 mmol) in DMF (10 ml) was added dropwise a solution of sodium thiomethoxide (343 mg, 4.9 mmol) in DMF (10 ml) under stirring at room temperature. After the mixture was stirred overnight, an additional sodium thiomethoxide (34 mg, 0.49 mmol) was added to the mixture. The reaction mixture was diluted with AcOEt and washed twice with H2O. The organic layer was dried over MgSO4 and evaporated to give 5-methylthio-2-nitro-N-[(1-diphenylmethylpiperidin-4-yl)methyl]benzamide as colorless powders, 1.7 g (80%): mp 179°-181° C.

1. stirringAfter the mixture was stirred overnight
2. washwashed twice with H2O
3. dry with materialThe organic layer was dried over MgSO4
4. customevaporated