Chemical Development of NBI-75043. Use of a Flow Reactor to Circumvent a Batch-Limited Metal− Halogen Exchange Reaction

…, S Chou, D Bonneville, RS Gross, P Wang…

Index: Gross, Timothy D.; Chou, Shine; Bonneville, Daniel; Gross, Raymond S.; Wang, Peng; Campopiano, Onorato; Ouellette, Michael A.; Zook, Scott E.; Reddy, Jayachandra P.; Moree, Wilna J.; Jovic, Florence; Chopade, Shubham Organic Process Research and Development, 2008 , vol. 12, # 5 p. 929 - 939

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Citation Number: 21

Abstract

Four types of histamine receptors have been characterized in humans (H1−H4).(1) The H1 receptor is the primary receptor involved in allergic rhinitis symptoms and motion sickness. H1 antagonists such as diphenhydramine hydrochloride block histamine binding in peripheral tissues, thereby reducing symptoms of allergic rhinitis.(2) One side effect of diphenhydramine results from its penetration of the blood−brain barrier resulting in CNS depression. Accordingly, selective ...