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Title: Resolution of 3-(methylamino)-1-(2-thienyl)propan-1-ol, a new key intermediate for duloxetine, with (S)-mandelic acid
Authors: Sakai, Kenichi
Sakurai, Rumiko
Yuzawa, Atsushi
Kobayashi, Yuka
Saigo, Kazuhiko
Issue Date: 20-Jun-2003
Publisher: Elsevier
Journal Title: Tetrahedron: Asymmetry
Volume: 14
Issue: 12
Start Page: 1631
End Page: 1636
Abstract: 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.
Rights: © 2003 Elsevier Science Ltd. All rights reserved.
DOI: http://dx.doi.org/10.1016/S0957-4166(03)00315-X
Type: Journal Article
URI: http://hdl.handle.net/10173/724
Appears in Collections:学術雑誌論文
西郷, 和彦 (SAIGO, Kazuhiko)

Please use this identifier to cite or link to this item: http://hdl.handle.net/10173/724

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