Preparation method of netarsudil key intermediate

• Main Authors: CHEN LEI, LIU YUXIAN, LU PINGBO, ZHANG WEIWEI, XING XIAOLAN
• Format: Patent
• Language: Chinese; English
• Published: 11.07.2017
• Subjects: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; 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; 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 provides a preparation method of a netarsudil key intermediate, and the netarsudil key intermediate is prepared from a benzyl alcohol derivative as a starting material in turn by benzyl alcohol group protection, carboxyl protecting, Henry reaction, dehydration for alkene formation, olefinic bond reduction, nitro reduction, amino protection and hydrolysis. The raw materials are cheap and easy to obtain, the reaction conditions are mild, the reaction controllability is high, and the method has good industrial application prospect. 本发明提供了种奈他地尔中间体的制备方法，具体而言，以苄醇衍生物为起始原料，经过苄醇基保护、羧基保护、Henry反应、脱水成烯、烯键还原、硝基还原、氨基保护、水解得到所需的中间体。本发明原料价廉易得，反应条件温和，反应可控性高，具有良好的工业化应用前景。