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

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.