反应详情

A mixture of 7.0 mg bistriphenylphosphinpalladium dichloride and 4 mg copperiodide in 5 ml triethylamine was heated to reflux for 30 min. To the resulting solution was added 0.41 g 5-bromo-6-(4-chloro-phenyl)-pyrazine-2-carboxylic acid ((R)-2-cyclopropyl-2-hydroxy-propyl)-amide (example 62 a) and 0.28 g triethylsilane and the mixture was refluxed for 0.5 h. The reaction mixture was cooled to room temperature and partitioned between 10% citric acid and ethyl acetate. The organic phase was purified by chromatography on silica gel with heptane:ethyl acetate=1:1 to yield 0.45 g of 6-(4-chloro-phenyl)-5-triethylsilanylethynyl-pyrazine-2-carboxylic acid ((R)-2-cyclopropyl-2-hydroxy-propyl)-amide as a solidifying foam.

1. temperaturewas heated
2. temperatureto reflux for 30 min
3. temperaturethe mixture was refluxed for 0.5 h
4. custompartitioned between 10% citric acid and ethyl acetate
5. customThe organic phase was purified by chromatography on silica gel with heptane