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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 41, 2011 - Issue 16
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Original Articles

Chemoenzymatic Route to S-Betaxolol

Yong-Hong Li New Drug Research and Development Center, Zhengzhou University, Zhengzhou, China; Department of Chemistry, Zhengzhou University, Zhengzhou, China
,
Li-Hua Huang New Drug Research and Development Center, Zhengzhou University, Zhengzhou, China; Department of Chemistry, Zhengzhou University, Zhengzhou, China
&
Hong-Min Liu New Drug Research and Development Center, Zhengzhou University, Zhengzhou, China; School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, ChinaCorrespondence[email protected]
Pages 2468-2474 | Received 03 Nov 2009, Published online: 14 Jun 2011
 
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Abstract

An efficient chemoenzymatic route to S-betaxolol is reported. A strain (Rhodotorula mucilaginosa DQ832198) screened from soil was used as biocatalyst for the kinetic resolution of the key acetylated intermediates. Excellent enantiomeric excess (ee > 99%) was obtained under very mild conditions. The biocatalyst is quite stable and could be used several times with little decrease of the resolving ability.

ACKNOWLEDGMENT

We acknowledge the National Natural Science Foundation of China for financial support of this work (20572103).

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