A Borrowing Hydrogen Approach to the Synthesis of RS-67,333

Abstract

A new strategy using the borrowing hydrogen methodology to access the 5-HT₄R agonist RS-67,333 is presented. Especially, this selective and highly potent ligand of 5-HT₄ receptor was obtained quickly and efficiently by catalytic alkylation of a ketone with various alcohols in the presence of a catalytic amount of (Cp*IrCl₂)₂.

Key words

iridium - catalysis - hydrogen transfer - alcohols - heterocycles

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