Synthesis of Macrolactams from Macrolactones Using Ru-/Ir-Catalytic System under Neutral Conditions

Herein, we report the Ru-/Ir-catalyzed synthesis of valuable macrolactams from macrolactones and esters. The ring-opening of the macrolactones was efficaciously facilitated by the Ru catalyst to generate 32 amides in the first step. In the second step, intramolecular N-alkylative ring closure of amides with alcohols was succeeded by Ir catalyst to provide a series of 22 macrolactams and gave water as a byproduct. Moreover, this approach proceeded under neutral conditions and avoided the use of external additives.