Preparation method of 4-hydroxyomeprazole

• Main Authors: YIN RENJIE, HE JIANXING, SUN WEI, SUN JIANMIN
• Format: Patent
• Language: Chinese; English
• Published: 02.02.2018
• Subjects: CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

The invention relates to a preparation method of an impurity 4-hydroxyomeprazole in the technical field of a medicament esomeprazole or omeprazole. The method specifically comprises the following steps: carrying out acid hydrolysis on omeprazole sulfide for demethylation, protecting phenolic hydroxyl group with acetic anhydride, oxidizing thioether with metachloroperbenzoic acid, and finally carrying out hydrolysis under an alkaline condition for deacetylation so as to obtain a target product. The method has short synthetic route and is simple to operate. The impurity product has high purity.The method can be applied in the research on omeprazole and esomeprazole impurity reference substances. 本发明涉及药物埃索美拉唑或奥美拉唑技术领域中种杂质：4-羟基奥美拉唑的制备方法。具体包括：将奥美拉唑硫醚酸水解脱去甲基，然后用乙酸酐保护酚羟基，间氯过氧苯甲酸氧化硫醚，最后碱性条件下水解脱去乙酰基，得到目标产物。本发明具有合成路线短，操作简便，所得杂质产物纯度高，可应用于奥美拉唑和埃索美拉唑杂质对照品研究等特点。