Synthesis of Haloperidol Using Enabling Technologies: Batch and Continuous Flow Studies

Haloperidol was discovered by Paul Janssen's research team in the late 1950s and significantly transformed the treatment of psychotic disorders, playing a crucial role in advancing biological psychiatry.¹ Industrially, its synthesis involves the condensation of a cyclic amine with a halogenated aromatic ketone, with two primary synthetic routes currently utilized for its production.^2,3 The present study aims to establish a new synthetic approach for haloperidol, beginning with simpler materials and incorporating continuous flow reactions and electrosynthesis.⁴ We have achieved relevant results in batch (Graphical Abstract), and we will now invest efforts to finish the synthesis and translate all the steps into continuous flow conditions.