Abstract We describe a new efficient synthesis of the prescribed racemic drug cetiedil [(±)-2- cyclohexyl-2-(3-thienyl) ethanoic acid 2-(hexahydro-1H-azepin-1-yl) ethylester]. Additionally, we report herein a high yielding large scale, route to its acid precursor 7, subsequently enabling large-scale synthesis of the chiral forms of cetiedil, and detailed pharmacological investigations.