新产品编号:905413

Chemical Name: N-[4(S)-[N-[2-(1-Naphtyl)acetyl]-3-methyl-L-valylamino]-3(R)-hydroxy-2(R)-(3,4,5-trimethoxybenzylamino)-5-phenylpentanoyl]-L-valine 2-hydroxy-4-methoxybenzylamide
CAS No. 376644-14-3
项目整合开发状态: Biological Testing
项目研究机构: Novartis (Originator)
合成路线:Condensation of glycidate (I) with 3,4,5-trimethoxybenzyl amine (II) in hot EtOH affords the hydroxy amino ester (III).Subsequent ester hydrolysis in (III) employing LiOH yields carboxylic acid (IV).This is coupled to N-2-hydroxy-4-methoxybenzyl-L-valinamide (V) by means of TPTU to furnish (VI).Then,removal of the N-Boc protecting group of (VI) with HCl in dioxane provides amine (VII).

合成路线:Coupling of N-Boc-L-tert-leucine (VIII) to amine (VII) in the presence of TPTU gives rise to amide (IX).After acidic Boc group cleavage in (IX),the resultant amine (X) is finally acylated by 1-naphthylacetic acid (XI) to furnish the title compound.