EDP-137

Chemical Name: 5-[(3aS,4S,6aR)-3a,4,6a-Trimethyl-2-oxoperhydrothieno[3,4-d]imidazol-4-yl]pentanoic acid 7-[N-[2-(2-azidophenyl)ethyl]-N-methylamino]-4-cyano-4-(3,4-dimethoxyphenyl)heptyl ester
项目整合开发状态: Biological Testing
项目研究机构: Universit?degli Studi di Firenze (Originator), Universit?Paris Nord (Originator)
合成路线:Acetonitrile derivative (I) is treated with BuLi and alkylated with 3-bromopropanol (A) to yield alcohol (II),which is further alkylated by means of LICKOR (n-BuLi/t-BuOK) and 1-chloro-3-bromopropane (B) to afford (III).Reaction of derivative (III) with secondary amine (VIII) in acetonitrile gives (IV).Amine (VIII) is obtained by trifluoroacetylation of azide (VI) with trifluoroacetic anhydride to yield (VII),which is then N-methylated by means of MeI and hydrolyzed with KOH.Finally,alcohol (IV) reacts with succinimido biotinate (V) in DMSO to provide the desired product.