Synthesis method of ticagrelor key intermediate

• Main Authors: HUANG RUOHE, SUN YONG, WU ZHENGHUA, LI ANPAI, JIANG JUNKANG, FENG YABING, ZHANG JIAQING
• Format: Patent
• Language: Chinese; English
• Published: 30.04.2021
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a synthesis method of a ticagrelor key intermediate, which belongs to the technical field of medical technologies, and is technically characterized by comprising the following steps: S1, dissolving a compound I in an organic solvent, adding strong base, reacting with sodium bromoacetate or bromoacetic acid, and adding ethyl chloroformate to synthesize a compound II; S2, adding sodium borohydride into the solution of the compound II in batches to obtain a compound III; and S3, deprotecting the compound III under the action of ammonium formate and 10% palladium on carbon, and then adding Ltartaric acid for salifying to synthesize a compound IV. The invention aims to provide a synthesis method of a ticagrelor key intermediate. The cost is effectively reduced, the synthesis process is simplified, and the method is suitable for large-scale production. 本发明公开了一种替卡格雷关键中间体的合成方法，其属于医药技术这一技术领域，技术要点包括：S1，化合物I溶于有机溶剂，加入强碱后与溴代乙酸钠或溴代乙酸反应，然后加入氯甲酸乙酯合成化合物II；S2，向上述化合物II的溶液中分批加入硼氢化钠，得到化合物III；S3，化合物III在甲酸铵和