Synthetic Story of a Blockbuster Drug: Reboxetine, a Potent Selective Norepinephrine Reuptake InhibitorClick to copy article linkArticle link copied!
Abstract
α-Aryloxybenzyl analogues of morpholine are a significant class of compounds because of their influence on the central nervous system (CNS), with particular concentration on their antidepressant potency. (±)-Reboxetine, an example of such α-aryloxybenzyl analogues, is an orally active and selective noradrenaline reuptake inhibitor that is presently recognized as a prescription drug in over 60 countries for depressive sickness and has been spaciously studied for its pharmacological characteristics. (+)-(S,S)-Reboxetine is presently undergoing advanced clinical evaluation as a potential treatment for neuropathic and fibromyalgia pain. Scheming well-organized approaches to access reboxetine and its derivatives represents a significant endeavor not only for developing antidepressant drugs but also advancing medical studies by radiolabeling of reboxetine derivatives with 11C, 18F, or 123I as potential positron emission tomography radioligands for imaging the brain norepinephrine transporter system. Therefore, to fulfill the challenge of creating the reboxetine architecture by improved synthetic routes, the review combines all of the literature synthetic processes for reboxetine and its derivatives on one platform. Cons and pros of each synthetic method are discussed in this review, which will be very fruitful for the synthetic and medical communities to increase the diversity of synthetic procedures and to develop new concepts and perceptions.
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