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Generated: August 22, 2017

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Title:Processes for preparing 3-benzazepines
Abstract: The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.
Inventor(s): Wolgast; Beverly L. (San Diego, CA), Gilson, III; Charles A. (San Diego, CA), Aytes; Shelley (San Diego, CA), Estrada; Scott A. (La Jolla, CA), Sengupta; Dipanjan (San Diego, CA), Smith; Brian (San Diego, CA), Rey; Max (Wallisellen, CH), Weigl; Ulrich (Hilzingen, DE)
Assignee: Arena Pharmaceuticals, Inc. (San Diego, CA)
Application Number:13/619,773
Patent Claims: 1. A composition comprising: a hydrochloric acid salt of a compound of Formula Va and a hydrochloric acid salt of a compound of Formula Vb, wherein the compound of Formula Va and the compound of Formula Vb have the structures, respectively, of ##STR00059## wherein R.sup.1 is H, R.sup.2 is Me, R.sup.3 is H, R.sup.4 is Cl, R.sup.5 is H, R.sup.6 is H, R.sup.8a is H, and R.sup.8b is H, and wherein the composition is enriched in the hydrochloric acid salt of the compound of Formula Vb.

2. The composition of claim 1, wherein the hydrochloric acid salt of the compound of Formula Vb is present in an enantiomeric excess of greater than about 80%.

3. The composition of claim 1, wherein the hydrochloric acid salt of the compound of Formula Vb is present in an enantiomeric excess of greater than about 90%.

4. The composition of claim 1, wherein the hydrochloric acid salt of the compound of Formula Vb is present in an enantiomeric excess of greater than about 95%.

5. The composition of claim 1, wherein the hydrochloric acid salt of the compound of Formula Vb is present in an enantiomeric excess of greater than about 98%.

6. The composition of claim 1, wherein the hydrochloric acid salt of the compound of Formula Vb is present in an enantiomeric excess of greater than about 99%.

7. The composition of claim 1, wherein the composition further comprises acetone.
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