新产品编号:755123
Chemical Name: N2-[4-(Benzyloxy)benzoyl]-N1-[2-(4-methoxyphenylamino)ethyl]-L-leucinamide
CAS No. 289044-26-4
项目整合开发状态: Biological Testing
项目研究机构: Novartis (Originator)
合成路线:Condensation of p-anisidine (I) with 2-oxazolidinone (II) in hot 2-(2-methoxyethoxy)ethanol affords the N-aryl ethanediamine (III).This is then coupled with the succinimidyl ester of N-Z-L-leucine (IV) to furnish amide (V).The N-carbobenzoxy group of (V) is further removed by catalytic hydrogenation,providing amine (VI),which is finally acylated by 4-(benzyloxy)benzoic acid (VII) by means of HATU to yield the title compound.
📌 参考资料/链接：
参考文献标题:Arylaminoalkylamides
文献作者:Missbach,M.; Altmann,E.; Lattmann,R.; Renaud,J.(Novartis AG)
参考来源:WO 0048993
📄 详细内容
合成路线:Condensation of p-anisidine (I) with 2-oxazolidinone (II) in hot 2-(2-methoxyethoxy)ethanol affords the N-aryl ethanediamine (III).This is then coupled with the succinimidyl ester of N-Z-L-leucine (IV) to furnish amide (V).The N-carbobenzoxy group of (V) is further removed by catalytic hydrogenation,providing amine (VI),which is finally acylated by 4-(benzyloxy)benzoic acid (VII) by means of HATU to yield the title compound.
参考文献标题:Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors
文献作者:Altmann,E.; Renaud,J.; Green,J.; Farley,D.; Cutting,B.; Jahnke,W.
参考来源:J Med Chem 2002,45(12),2352