title: Application of kinetic resolution using HCS as chiral auxiliary: novel synthesis of beta-blockers (S)-betaxolol and (S)-metoprolol.
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.
authors.affiliation: New Drug Research & Development Center, Zhengzhou University, Zhengzhou, People's Republic of China.
authors.forename: Jing-Yu
authors.initials: JY
authors.lastname: Zhang
authors.forename: Hong-Min
authors.initials: HM
authors.lastname: Liu
authors.forename: Xiao-Jun
authors.initials: XJ
authors.lastname: Wang
authors.forename: Pei
authors.initials: P
authors.lastname: Wang
authors.forename: Jia-Xin
authors.initials: JX
authors.lastname: Zheng
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis* / Q000737:chemistry; D015784:Betaxolol / Q000138:chemical synthesis* / Q000737:chemistry; D007700:Kinetics; D008790:Metoprolol / Q000138:chemical synthesis* / Q000737:chemistry; D015394:Molecular Structure; D013237:Stereoisomerism
chemical_list: D000319:Adrenergic beta-Antagonists; D008790:Metoprolol; D015784:Betaxolol