METHOD FOR PREPARING POTASSIUM ION COMPETITIVE BLOCKER INTERMEDIATE

A method for synthesizing a key intermediate compound 1 of fexuprazan, which is a potassium ion competitive blocker. The method comprises using 2,4-difluorobenzylamine as a raw material, and sequentially conducting condensation reaction, benzyl protection, ring formation under basic conditions, meth...

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Bibliographic Details
Main Authors HUANG, Zhining, MI, Chenggen, ZHOU, Zhangtao, PHILLIS, Andrew Toroa, YE, Weiping, YANG, Manxin
Format Patent
LanguageChinese
English
French
Published 17.03.2022
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:A method for synthesizing a key intermediate compound 1 of fexuprazan, which is a potassium ion competitive blocker. The method comprises using 2,4-difluorobenzylamine as a raw material, and sequentially conducting condensation reaction, benzyl protection, ring formation under basic conditions, methylation, deprotection, and the like to obtain a target product. The described method has a yield greater than 50% and has characteristics such as mild reaction conditions, low costs, and the like. Procédé de synthèse d'un composé intermédiaire clé 1 de fexuprazan, qui est un bloqueur compétitif d'ions de potassium. Le procédé comprend l'utilisation de 2,4-difluorobenzylamine en tant que matière première et la réalisation séquentielle d'une réaction de condensation, d'une protection de benzyle, d'une formation d'anneau dans des conditions basiques, d'une méthylation, d'une déprotection et similaires pour obtenir un produit cible. Le procédé décrit a un rendement 50 % supérieur et présente des caractéristiques telles
Bibliography:Application Number: WO2020CN114470