Optimization and Scale-up of a Pd-Catalyzed Aromatic C− N Bond Formation: A Key Step in the Synthesis of a Novel 5-HT1B Receptor Antagonist

HJ Federsel, M Hedberg, W Tian

Index: Federsel, Hans-Juergen; Hedberg, Martin; Qvarnstroem, Fredrik R.; Tian, Wei Organic Process Research and Development, 2008 , vol. 12, # 3 p. 512 - 521

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Citation Number: 22

Abstract

Searching for the best synthetic route for a given target molecule is a complex task and, by the same token, a key deliverable from a process R&D department. In this vein the challenge for our group was to identify a sustainable manufacturing process for a chiral compound, AR- A2, to be developed for the treatment of certain neurological disorders. Besides designing a method for assembling the core (R)-2-aminotetralin nucleus, a key feature in the overall ...