Direct Resolution of the Enantiomers of Betaxolol and Related Intermediates, and Its Application |
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| Authors: | Yong-Hong Li Li-Hua Huang Shu-Sheng Zhang Hong-Min Liu |
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| Affiliation: | 1. Department of Chemistry, School of Pharmaceutical Sciences, New Drug Research and Development Center, Zhengzhou University, Zhengzhou, 450001, People’s Republic of China
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| Abstract: | An OJ-H chiral column has been used for direct resolution of the enantiomers of betaxolol and related intermediates in the preparation of (S)-betaxolol. The enantiomers can be excellently resolved (R S > 2) within 9.4 min with high peak symmetry. The enantiomers of some acetylated intermediates, which cannot be resolved on an OD-H column, can also be resolved. The method is simple and suitable for routine determination of ee values in the preparation of (S)-betaxolol. |
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