- First scale-up: Problems and resolutions on the synthesis of WAY-253752, a novel, dual-acting SSRI/5HT1A antagonist
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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.
- Nikitenko, Antonia,Evrard, Deborah,Sabb, Annmarie L.,Vogel, Robert L.,Stack, Gary,Young, Mairead,Lin, Melissa,Harrison, Boyd L.,Potoski, John R.
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- CYCLOALKYLFUSED INDOLE, BENZOTHIOPHENE, BENZOFURAN AND INDENE DERIVATIVES
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The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central nervous system diseases by antagonizing 5-HT1A receptors and mo
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(2008/06/13)
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