Synthesis of 3-hydroxy desloratadine, the hydroxyl metabolite of loratadine


ABSTRACT:

Allergic rhinitis (AR) is an IgE-mediated disease that can impact the quality of life and work of affected individuals. Antihistamines were introduced more than 50 years ago for the treatment of AR. They can be classified into three groups. First-generation antihistamines such as promethazine and ketotifen are clinically effective, but they have a considerably limited use by their sedative and anticholinergic effects. Second-generation antihistamines such as cetirizine, loratadine1 and mizolastine have significantly fewer sedative and anticholinergic effects than first-generation. New generation antihistamines include fexofenadine, levocetirizine, desloratadine2 and rupatadine. While many of these agents were largely devoid of CNS (central nervous system) side effects, their tendency for drug-drug interactions (e.g., terfenadine and astemizole) resulted in an increase incidence of cardiotoxicity. Furthermore, some of the second-generation H1 antagonists exhibited weak anti-inflammatory properties and had no effect on nasal congestion. These observations emphasized the need for newer anti-allergic agents with a potent and long lasting activity, low liability to enter into the brain and lacking cardiotoxic potential.

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