Application of kinetic resolution using HCS as chiral auxiliary: novel synthesis of beta-blockers (S)-betaxolol and (S)-metoprolol |
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| Authors: | Zhang Jing-Yu Liu Hong-Min Wang Xiao-Jun Wang Pei Zheng Jia-Xin |
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| Affiliation: | New Drug Research & Development Center, Zhengzhou University, Zhengzhou, People's Republic of China. |
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| Abstract: | Optically pure (S)-betaxolol and (S)-metoprolol were prepared with an extremely facile and practical method using kinetic resolution of beta-amino alcohols employing HCS as chiral auxiliary. High enantiomeric purity (ee > 99%) was achieved and the synthetic strategy is amenable to industrial scale-up. |
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| Keywords: | resolution synthesis (S)‐betaxolol (S)‐metoprolol |
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