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1134010 学術雑誌論文 >
Please use this identifier to cite or link to this item:
http://hdl.handle.net/2261/3990
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| タイトル: | Resolution of 3-(methylamino)-1-(2-thienyl)propan-1-ol, a new key intermediate for duloxetine, with (S)-mandelic acid |
| 著者: | Saigo, Kazuhiko
Sakai, Kenichi
Sakurai, Rumiko
Yuzawa, Atsushi
Kobayashi, Yuka |
| 著者(別言語): | 西郷, 和彦 |
| Issue Date: | 20-Jun-2003 |
| 出版者: | Elsevier |
| 掲載誌情報: | Tetrahedron: Asymmetry, 14(12), 2003, p. 1631-1636. |
| Relation URI: | http://www.sciencedirect.com/science/journal/09574166 |
| 抄録: | The resolution of racemic 3-(methylamino)-1-(2-thienyl)propan-1-ol (3), a new key intermediate for duloxetine (1), was studied. The conditions were optimized for an industrial-scale resolution of 3 by using (S)-mandelic acid (4) as a resolving agent and 2-butanol containing two equimolar amounts of water as a solvent. The (S)-3･(S)-4･H2O diastereomeric salt was crystallized to give pure (S)-3 with >99.9% ee after liberation of the amine. Absolute configuration of liberated (-)-3 was determined as (S)-form by X-ray crystallography. |
| URI: | http://hdl.handle.net/2261/3990 |
| ISSN: | 09574166 |
| Appears in Collections: | 1134010 学術雑誌論文
014 自然科学
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