Synthesis of active pharmaceutical ingredient atomoxetine via desulfurative halogenation

An innovative preparation of the Active Pharmaceutical Ingredient (API) Atomoxetine has been developed. Key advantages of the synthetic procedure include: a one-pot preparation of a 1,3-bis-electrophilic phenyl-propionic synthon obtained via desulfurative chlorination of an easy to make thiophenyl sulfide; an unreported strategy for the preparation of secondary amines. The synthesis involves a total of four consecutive steps from unexpensive and readily available reagents and employes mild conditions. • A four steps synthesis of Atomoxetine has been realized via (i) designing a 1,3-bis-electrophile; optimising a procedure to prepare the 1,3-bis electrophile in a single operation; (iii) optimising Gabriel's synthesis to prepare secondary amines.