新产品编号:1924221

Chemical Name: 1-(Aminomethyl)-6,8-dimethoxyisoquinoline-4-carboxylic acid ethyl ester dihydrochloride
项目整合开发状态: Biological Testing
项目研究机构: Novartis (Originator)
合成路线:Acylation of ethyl 3-amino-2-(3,5-dimethoxyphenyl)propionate (I) with N-phthaloylglycine (II) using EDC and HOAt afforded amide (III),which was subjected to a Bischler-Napieralski cyclization in the presence of POCl3 to produce the dihydroisoquinoline (IV).Aromatization of (IV) to the corresponding isoquinoline (V) was achieved by treatment with MnO2 in refluxing benzene.Hydrazinolysis of the phthaloyl group of (V) gave the free amine,which was purified after conversion to the N-Boc derivative (VI).Acid cleavage of the Boc group then furnished the title product.