【药物名称】EDP-137
化学结构式(Chemical Structure):
参考文献No.552005
标题:Synthesis and binding properties of photoactivable biotin-conjugated verapamil derivatives for the study of P-170 glycoprotein
作者:Teodori, E.; Ettori, D.; Garnier-Suillero, A.; Gualtieri, F.; Manetti, D.; Romanelli, M.N.; Scapecchi, S.
来源:Bioorg Med Chem 1999,7(9),1873
合成路线图解说明:

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.

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