Ruthenium-Catalyzed Regioselective Synthesis of C3-Alkylated Indoles Following Transfer Hydrogenation or Borrowing Hydrogen Strategy

Abstract

By employing either borrowing hydrogen or transfer hydrogenation strategy, two straightforward [Ru(p-cymene)Cl₂]₂-catalyzed methods for regioselective synthesis of C3-alkylated indoles have been developed, utilizing alcohols as H atom donors or alkylating agents. The developed catalytic system could accommodate a broad substrate scope including primary/secondary aliphatic alcohols and substituted indoles, and in most cases providing good yields. Notable features of the developed system include high-activity, easy operation, and air atmosphere.

Key words

transfer hydrogenation - borrowing hydrogen - alkylation - indoles - alcohols

Publication History

Received: 01 December 2022

Accepted after revision: 22 December 2022

Accepted Manuscript online:
22 December 2022

Article published online:
12 January 2023

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