反应详情

To a solution of 2-((3-amino-2-cyanophenoxy)methyl)-N-ethylpiperidine-1-carboxamide (Example 26b. 0.407 g, 1.35 mmol) in DMA (5 mL) was added sulfamoyl chloride (0.234 mg, 2.02 mmol) and the reaction mixture was stirred vigorously at r.t. for 2 h, then extracted with H2O/EtOAc. The combined organic phases were washed with brine, dried over MgSO4, filtered and evaporated. The residue was purified by Biotage purification system (120 g Silicycle column, DCM:THF=4:1 as eluent) to provide the desired product (0.606 g, 90%). MS 382 (MH+).

1. extractionextracted with H2O/EtOAc
2. washThe combined organic phases were washed with brine
3. dry with materialdried over MgSO4
4. filtrationfiltered
5. customevaporated
6. customThe residue was purified by Biotage purification system (120 g Silicycle column, DCM:THF=4:1 as eluent)