反应详情

130 mg of 2-[[(1,2-dihydro-2-oxopyridin-4-yl)methyl]amino]-N-(isoquinolin-3-yl)benzoic acid amide is introduced into 4 ml of a mixture that consists of toluene:methanol=1:3.5 and mixed with 0.2 ml of a 2-molar solution of trimethylsilyldlazomethane in hexane and stirred for 8 hours at room temperature. After repeated addition of 0.2 ml of trimethylsilyldiazomethane solution and 1 hour of stirring, the batch is evaporated to the dry state and chromatographed on silica gel with methylene chloride:ethanol=97:3 as an eluant. 20 mg of 2-[(−2-methoxypyridin-4-yl)methyl]amino]-N-(isoquinolin-3-yl)benzic acid amide and 10 mg of 2-[[(1,2-dihydro-1-methyl-2-oxopyridin-4-yl)methyl]amino]-N-(isoquinolin-3-yl)-benzoic acid amide are obtained.

1. stirringof stirring
2. customthe batch is evaporated to the dry state
3. customchromatographed on silica gel with methylene chloride