反应详情

温度

50 °C

134 μl (1.3 mmol) thiophenemethanamine, 438 mg (1.1 mmol) HATU and 420 μl (3.0 mmol) NEt3 were added in succession to a solution of 330 mg (1.05 mmol) 2-(ethylthio)-4-methyl-7-(trifluoromethyl)quinoline-3-carboxylic acid (VVV08) in THF (8 ml) and the mixture was then heated for 24 h at 50° C. Then it was diluted with EE and washed with a 4M aqueous NH4Cl solution, a 1M aqueous Na2CO3 solution and brine. The organic phase was dried over MgSO4 and then filtered through a silica layer. Column chromatography (hexane/EE 7:3) of the residue yielded 277 mg (0.67 mmol, 65%) 2-ethylsulfanyl-4-methyl-N-(thiophen-2-yl-methyl)-7-(trifluoromethyl)-quinoline-3-carboxamide. MS: m/z 411.1 [M+H]+.

1. additionThen it was diluted with EE
2. washwashed with a 4M aqueous NH4Cl solution
3. dry with materialThe organic phase was dried over MgSO4
4. filtrationfiltered through a silica layer