帕金森病治疗用药物罗替戈汀的合成新工艺  

New Synthesis Technology of Rotigotine as a Drug for the Treatment of Parkinson's Disease

作　　者：樊燕鸽[1] 李峥 赵俊宏[1] 王红星 薛宝玉[1] FAN Yange;LI Zheng;ZHAO Junhong;WANG Hongxing;XUE Baoyu(Institute of Chemistry Co.Ltd.,Henan Academy of Sciences,Zhengzhou 450002,China)

机构地区：[1]河南省科学院化学研究所有限公司,郑州450002

出　　处：《河南科学》2019年第3期381-386,共6页Henan Science

基　　金：河南省科技攻关项目(172102310341)

摘　　要：通过5-甲氧基-2-四氢萘酮为原料制备出亚胺,再以汉斯酯1,4-二氢吡啶(HEH)为还原剂,以手性磷酸为催化剂合成立体结构单一的重要中间体(S)-2-(N-正丙基)氨基-5-甲氧基四氢萘,再进一步合成罗替戈汀.经过红外吸收光谱、高效液相色谱(HPLC)、核磁共振碳谱、核磁共振氢谱分析表征合成物质结构,说明合成的物质为罗替戈汀.此合成工艺是以立体选择性化学反应合成专一立体结构的化合物,制备工艺简便,产品收率高.The imine was prepared from 5-methoxyl-2-tetrahydronaphone,Hantzsch ester 1,4-dihydropyridine(HEH)is used as reducing agent,and chiral phosphoric acid is used as catalyst to synthesize single important intermediate of stereostructure.Rotigotine is further synthesized by this intermediate S(-)2-(N-propylamino)-5- methoxytetralin.The structures of the synthesized compounds were characterized by Infrared Spectrum,High Performance Liquid Chromatograph,Nuclear Magnetic Resonance Carbon Spectroscopy and Nuclear Magnetic Resonance Hydrogen Spectroscopy.The synthetic process is a stereoselective chemical reaction for the synthesis of a specific solid structure.The preparation process is simple and the yield is high.

关 键 词：5-甲氧基-2-四氢萘酮 立体选择性 合成 罗替戈汀 

分 类 号：O69[理学—化学] R97.5[医药卫生—药品]