Production method of substance relative to anticoagulant Apixaban

• Main Authors: ZHU WANJIANG, DOU XIAOWEI, XING JUNHAO
• Format: Patent
• Language: Chinese; English
• Published: 03.12.2019
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a production method of a substance relative to anticoagulant Apixaban. The method comprises the following steps: with ethyl 6-(4-aminophenyl)-1-(4-methoxyphenyl)-7-oxo-4,5-dihydropyrazolo[3,4-c]pyridine-3-carboxylate as a raw material, subjecting the ethyl 6-(4-aminophenyl)-1-(4-methoxyphenyl)-7-oxo-4,5-dihydropyrazolo[3,4-c]pyridine-3-carboxylate and ethyl 4-acetylbutyrateto a reductive amination reaction to obtain a compound III; under the action of an alkali, subjecting the compound III to intramolecular cyclization to obtain a compound VII; and subjecting an estergroup in the structure of the compound VII to an aminolysis reaction to obtain a final product II. The synthesis method has the characters that the raw materials are cheap and easy to obtain, the total yield is high, the route is short, and the like, so that material guarantee is provided for subsequent quality control studies and safety property studies in a production process of the Apixaban. 本发明公开了一种抗凝药物阿哌沙班相关物质的制备方法。该方