Ir-Catalyzed Synthesis of Functionalized Pyrrolidines and Piperidines Using the Borrowing Hydrogen Methodology

The Ir(III)-catalyzed synthesis of 3-pyrrolidinols and 4-piperidinols combining 1,2,4-butanetriol or 1,3,5-pentanetriol with primary amines was carried out. This borrowing hydrogen methodology was further extended to the sequential diamination of triols leading to amino-pyrrolidines and aminopiperidines.

Automated summary

In this study, the Ir(III)-catalyzed synthesis of 3-pyrrolidinols and 4-piperidinols by reacting 1,2,4-butanetriol or 1,3,5-pentanetriol with primary amines was demonstrated. This borrowing hydrogen methodology was also applied to the sequential diamination of triols, leading to the formation of amino-pyrrolidines and aminopiperidines.