Preparation method of (S)-2-amino-2-(3-fluoro-5-methoxyphenyl) ethanol hydrochloride

The invention relates to the field of pharmaceutical chemical industry, in particular to a preparation method of (S)-2-amino-2-(3-fluoro-5-methoxyphenyl) ethanol hydrochloride, which is a high-selectivity asymmetric synthesis method, that is, aldehyde is subjected to Grignard reagent addition, oxida...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: CHAI BAOHONG, WEN ZHAOFENG, KAI YONGPING, LU GANG
Format: Patent
Sprache:chi ; eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The invention relates to the field of pharmaceutical chemical industry, in particular to a preparation method of (S)-2-amino-2-(3-fluoro-5-methoxyphenyl) ethanol hydrochloride, which is a high-selectivity asymmetric synthesis method, that is, aldehyde is subjected to Grignard reagent addition, oxidation, alpha-bromination, acetyl esterification and hydrolysis to obtain a hydroxyl ketone intermediate, and the hydroxyl ketone intermediate is subjected to hydrolysis to obtain the (S)-2-amino-2-(3-fluoro-5-methoxyphenyl) ethanol hydrochloride. The hydroxyl of the ketone intermediate is protected by TPSCl, the ketone intermediate and a chiral induction reagent are subjected to dehydration condensation to produce Schiff base, a high-selectivity chiral intermediate is obtained through a reduction reaction, and a target compound can be obtained through a protection group removal reaction and acidolysis. 本发明涉及医药化工领域,具体来说,涉及一种(S)-2-氨基-2-(3-氟-5-甲氧基苯基)乙醇盐酸盐的制备方法,其是一种高选择性的不对称合成方法,即醛经过格氏试剂加成、氧化、α-溴代,乙酰基酯化、水解得到羟基酮类中间体,该酮类中间