Optically active ilaprazole and synthesis method thereof

• Main Authors: ZHOU ZHANGTAO, YE WEIPING, MO AILI, XU JUNYE, YAN YANNAN, FEI ANJIE
• Format: Patent
• Language: Chinese; English
• Published: 23.10.2018
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention relates to optically active ilaprazole and a synthesis method thereof, belongs to the field of pharmaceutical technology, and discloses a method for synthesizing optically active ilaprazole. According to the method, corresponding thiol is used as a starting raw material, and reacts with acrylate or halopropionate to obtain a thioether compound, the thioether compound is oxidized to obtain racemic sulfoxide, and the racemic sulfoxide reacts with another fragment under the action of a chiral phase transfer catalyst to obtain the chiral ilaprazole. According to the present invention, the preparation of the chiral ilaprazole is firstly reported, the synthesis method of the chiral ilaprazole does not require the use of heavy metals and the use of dangerous peroxides, and the excessive oxidation by-product is generated at the penultimate chemical step so as to easily control; and the method has characteristics of novel process, few steps, mild reaction conditions and the like. 种光学活性艾普拉唑及其合成方法，属于制药技术领域