| Item type |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2011-08-30 |
| タイトル |
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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 |
| 言語 |
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言語 |
eng |
| 資源タイプ |
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|
資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
|
資源タイプ |
journal article |
| 著者 |
Sakai, Kenichi
Sakurai, Rumiko
Yuzawa, Atsushi
Kobayashi, Yuka
Saigo, Kazuhiko
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| 抄録 |
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内容記述タイプ |
Abstract |
|
内容記述 |
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. |
| 書誌情報 |
Tetrahedron: Asymmetry
巻 14,
号 12,
p. 1631-1636,
発行日 2003-06-20
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| ISSN |
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収録物識別子タイプ |
ISSN |
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収録物識別子 |
0957-4166 |
| 書誌レコードID |
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収録物識別子タイプ |
NCID |
|
収録物識別子 |
AA1074621X |
| DOI |
|
|
関連タイプ |
isVersionOf |
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|
識別子タイプ |
DOI |
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関連識別子 |
10.1016/S0957-4166(03)00315-X |
| 権利 |
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|
権利情報 |
© 2003 Elsevier Science Ltd. All rights reserved. |
| 著者版フラグ |
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出版タイプ |
AM |
|
出版タイプResource |
http://purl.org/coar/version/c_ab4af688f83e57aa |
| 出版者 |
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出版者 |
Elsevier |
| 関係URI |
|
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識別子タイプ |
URI |
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関連識別子 |
http://www.sciencedirect.com/science/journal/09574166 |
|
|
関連名称 |
http://www.sciencedirect.com/science/journal/09574166 |
ttrasy_14_1631.pdf (146.3 kB)
