反应详情

温度

100 °C

3-[3-[[1-[2-(2-Chloroethoxy)phenyl]-1-methylethyl]amino]-2-oxo-1(2H)-pyrazinyl]-N-cyclopropyl-4-methyl-benzamide (Example 198e, 17.5 g) in dioxane (50 mL) was treated with 40% Methylamine solution (50 mL) under nitrogen. The resulting suspension was heated in a sealed system at 100° C. for 4 h. After cooling to room temperature, the solution was evaporated to dryness. The crude product was purified by flash chromatography (SiO2, eluent 10% methanol in dichloromethane and 1% triethylamine). Evaporation of the relevant fractions to dryness and trituration of the residue in diethyl ether gave a solid which was filtered off and dried to give the title compound (12.5 g) as an off white solid.

1. temperatureAfter cooling to room temperature
2. customthe solution was evaporated to dryness
3. customThe crude product was purified by flash chromatography (SiO2, eluent 10% methanol in dichloromethane and 1% triethylamine)
4. customEvaporation of the relevant fractions to dryness and trituration of the residue in diethyl ether
5. customgave a solid which
6. filtrationwas filtered off
7. customdried