茚达特罗的中间体5,6-二乙基-2,3-二氢-1H-茚-2-胺盐酸盐的合成

茚达特罗的中间体5,6-二乙基-2,3-二氢-1H-茚-2-胺盐酸盐的合成 Synthesis of Indacaterol Intermediate 5,6-Diethyl-2,3-Dihydro-1H-Inden-2-Amine Hydrochloride 蔡丽华 CAI Lihua 1 first-author 杜小兰 DU Xiaolan 2 孙大成 SUN Dacheng 2 武汉长江工商学院工学院 武汉长江工商学院工学院 Wuhan Vanz Pharm Inc Wuhan Vanz Pharm Inc 武汉万知生物医药有限公司 武汉万知生物医药有限公司 College of Engineering,Wuhan Yangtze Business University College of Engineering,Wuhan Yangtze Business University 以易得且廉价的乙苯为起始原料合成了茚达特罗的中间体5,6-二乙基-2,3-二氢-1H-茚-2-胺盐酸盐.该合成方法分8个步骤:氯丙酰化、环化、肟化、钯炭氢化还原、氨基保护、乙酰化、还原、去保护并成盐,得到最终产品.产品通过元素分析、质谱及核磁共振等测试手段进行了表征. An efficient and economical synthesis of 5,6-diethyl-2,3-dihydro-1H-inden-2-amine hydrochloride utilizing ethylbenze as a cheap and commercially readily available starting material is described.The newly developed synthesis involves eight-steps:chlorpromazine acylated,cyclization,oximation,hydrogenation using Pd/C catalyst,amino-protecting,acetylation,hydrogenation,deprotection and salt.The complexes were characterized by elemental analysis,MS and 1 H NMR. 茚达特罗 乙苯 5,6-二乙基-2,3-二氢-1H-茚-2-胺盐酸盐 合成 indacaterol ethylbenzene 5,6-diethyl-2,3-dihydro-1H-inden-2-amine hydrochloride synthesis 10.14188/j.1671-8836.2014.03.015 O621.3 国家自然科学基金资助项目（20575047） 2014-03-01 2021-04-01 3 60