Efficient access to multi-substituted 1-aminoisoquinolines via Rh(III)-catalyzed oxidative annulation of aminopyridine pivalamides with internal alkynes

The synthesis of multi-substituted 1-aminoisoquinolines from aminopyridine pivalamides with alkynes by Rh(III)-catalyzed C–H activation coupling has been investigated. This method proved to be tolerant of synthetically versatile functional groups, and provided access to a few highly substituted isoquinoline derivatives with remarkable fluorescence properties in moderate yields.