新产品编号:1251871

Chemical Name: N,N'-Bis[2-(fluorenyl-9-ylmethoxycarbonyl)-1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl]-2,2-(diamino)ethanol
项目整合开发状态: Biological Testing
项目研究机构: Universit?di Ferrara (Originator)
合成路线:The Hofmann degradation of dipeptide amide (I) using bis(trifluoroacetoxy)iodobenzene in aqueous acetonitrile yielded the geminal diamine derivative (II).After deprotection of the tert-butyl group of (II) with aqueous trifluoroacetic acid containig anisole,the resulting aminoalcohol (III) was coupled with N-(benzyloxycarbonyl) tetrahydroisoquinoline-3-carboxylic acid (IV) by means of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide-HCl (EDC) and 1-hydroxy- benzotriazole (HOBt) to afford the geminal diamide (V).The catalytic hydrogenolysis of both benzyloxycarbonyl groups of (V) was carried out in the presence of Pd/C,and the deprotected diamino compound (VI) was finally converted to the bis(Fmoc) derivative by coupling with N-(9-fluorenylmethoxycarbonyloxy)succinimide (VII) in the presence of N-methylmorpholine.