Synthesis preparation method of rivaroxaban key intermediate

• Main Authors: CHAO HU, FAN WANG, SONG LIN, XIAO-HU FENG, ZAI-XIN CHEN, ZHENG-JUN XIA, BIN WANG, SHUI-TAO YU
• Format: Patent
• Language: English
• Published: 22.07.2015
• 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 discloses a synthesis preparation method of a key intermediate for synthesizing rivaroxaban as shown in formula I. The preparation method comprises the following steps: using compounds as shown in formulae II and III as the initial raw materials, performing condensation and cyclization, hydrolysis, oxidation and reductive amination to obtain the key intermediate for synthesizing rivaroxaban as shown in the formula I. The preparation method has the characteristics of being mild in reaction conditions, simple and convenient in process operation, high in stability and controllability, high in atom utilization ratio, environment-friendly, and low in production cost, is suitable for industrial mass production.