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

作　　者：蔡丽华[1] 杜小兰 孙大成 

机构地区：[1]武汉长江工商学院工学院,湖北武汉430065 [2]武汉万知生物医药有限公司,湖北武汉430056

出　　处：《武汉大学学报（理学版）》2014年第3期279-282,共4页Journal of Wuhan University:Natural Science Edition

基　　金：国家自然科学基金资助项目(20575047)

摘　　要：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-lH-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, ami- no-protecting, acetylation, hydrogenation, deprotection and salt. The complexes were characterized by elemental analysis, MS and ^1 H NMR.

关 键 词：茚达特罗 乙苯 5 6-二乙基-2 3-二氢-1H-茚-2-胺盐酸盐 合成 

分 类 号：O627.41[理学—有机化学]