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First Scale-Up: Problems and Resolutions on the Synthesis of WAY-253752, a Novel, Dual-Acting SSRI/5HT1A Antagonist

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journal contribution
posted on 18.01.2008, 00:00 by Antonia Nikitenko, Deborah Evrard, Annmarie L. Sabb, Robert L. Vogel, Gary Stack, Mairead Young, Melissa Lin, Boyd L. Harrison, John R. Potoski
An alternative synthesis of WAY-253752, 1, a novel, dual-acting SSRI/5HT1A antagonist, was developed and used for the first scale-up. Initially, the target compound was synthesized as part of a diasteromeric mixture separated by chiral preparative HPLC. The new route was designed around intermediates suitable for chiral resolution, and its conditions were successfully determined.