反应详情

温度

60 °C

A mixture of 0.212 g (0.707 mmol) 6-bromo-5-piperidin-1-yl-pyrazine-2-carboxylic acid methyl ester, 0.006 g (0.778 mmol) isopropanol and 0.034 g (0.778 mmol) NaH (55% dispersion in oil) in 1.7 mL dioxane was heated to 60° C. for 16 h. Water and 5N KOH was added and the mixture was heated to 50° C. for 4 h. Formic acid and DMF was added and the mixture was subjected to purification by preparative HPLC on reversed phase eluting with a gradient formed from acetonitrile, water and formic acid. The product fractions were combined and evaporated to yield 0.04 g (21%) of the title compound. m/z (ES+): 266.4 (M+H).

1. temperaturethe mixture was heated to 50° C. for 4 h
2. customthe mixture was subjected to purification by preparative HPLC on reversed phase
3. washeluting with a gradient
4. customformed from acetonitrile, water and formic acid
5. customevaporated