1-(Arylsulfonyl)cyclopropanol, a new cyclopropanone equivalent and its application to prepare 1-alkynyl cyclopropylamine

Cyclopropanone derivative 1-(arylsulfonyl)cyclopropanol 4 simply prepared from the reaction of cyclopropanone ethyl hemiacetal 3 with sodium arylsufinate in the presence of formic acid is a new cyclopropanone equivalent to react with terminal acetylenes, and disubstituted amines in water catalyzed by AuCl3, to provide an unprecedented synthesis of 1-alkynyl cyclopropylamines in moderate yields.

Graphical abstract1-(Arylsulfonyl)cyclopropanol 4, a new cyclopropanone equivalent, can react with terminal acetylenes, and disubstituted amines in water catalyzed by AuCl3, to provide 1-alkynyl cyclopropylamines in moderate yields.Figure optionsDownload full-size imageDownload as PowerPoint slide