Work

Selective Organocatalytic Synthesis of 3‐Methylindoles and Diindolylmethanes through Reductive Methylation of Indoles with CO2

Year: 2025

Type: article

Abstract: The direct reductive methylation of indoles with CO2 remains a formidable challenge due to competing reduction pathways and precise selectivity control. Herein, cooperative catalytic systems comprising 2‐aminopyridine–BH3 and DIC–BH3 are disclosed, which enable unprecedented chemoselective C3‐methylation of indoles under mild conditions (1 atm CO2). This strategy delivers two distinct product classes through controlled reduction: 3‐methylindoles (up to 81% yield) and diindolylmethanes (up to 82% yield) with excellent functional group tolerance. This protocol offers novel synthetic routes for the synthesis of indole‐based bioactive molecules.

Source: ChemSusChem

DOI: 10.1002/cssc.202500594

Authors: He Zhang, Rongpei Wu, Ke Gao

Institution: Central China Normal University

Language: English

Topic: Carbon dioxide utilization in catalysis

Subfield: Process Chemistry and Technology

Field: Chemical Engineering

Domain: Physical Sciences

SDG: Climate action

Open Access status: bronze

Funders: National Natural Science Foundation of China, Central China Normal University, Project 211, Fundamental Research Funds for the Central Universities