反応 #2054464

反応方程式

cesium carbonate

(6S)-7-(tert-butyldimethylsilyloxy)-6-methyl-5-azaspiro[2.4]heptan-4-one

4,5-bis(diphenylphosphino)-9,9-dimethylxanthene

4-iodo-2-trifluoromethylbenzonitrile

→

title compound

収率 56.0%

4-[(6S,7R)-7-(tert-butyldimethylsilyloxy)-6-methyl-4-oxo-5-azaspiro[2.4]hept-5-yl]-2-(trifluoromethyl)benzonitrile

収率 56.0%

4-[(6S,7S)-7-(tert-butyldimethylsilyloxy)-6-methyl-4-oxo-5-azaspiro[2.4]hept-5-yl]-2-(trifluoromethyl)benzonitrile

収率 26.0%

反応条件

実験手順

Using (6S)-7-(tert-butyldimethylsilyloxy)-6-methyl-5-azaspiro[2.4]heptan-4-one (720.5 mg), 4-iodo-2-trifluoromethylbenzonitrile (921.3 mg), cesium carbonate (1.38 g), tris(dibenzylideneacetone)dipalladium(0) (129 mg) and 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (326 mg), and in the same manner as in Reference Example 3, the title compound (yield: 670 mg, yield 56%) and 4-[(6S,7S)-7-(tert-butyldimethylsilyloxy)-6-methyl-4-oxo-5-azaspiro[2.4]hept-5-yl]-2-(trifluoromethyl)benzonitrile (yield: 309 mg, 26%) were obtained each as a colorless solid.

出典