Preparation of lidocaine, bipuvacaine, mepivacaine, trimecaine, and pyromecaine by reductive acylation on palladium catalysts

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Abstract

A method for the catalytic synthesis of local anesthetics — lidocaine, bipuvacaine, mepivacaine, trimecaine, and pyromecaine — by reductive acylation is described. The process takes place in mild conditions (20–50°C, hydrogen at atmospheric pressure, organic solvent) with target product yields of 54–93%.

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