新产品编号:2406731
Chemical Name: N1-[3-[2-Amino-1(S)-(biphenyl-4-ylmethyl)-2-oxoethylamino]-1(S)-benzyl-2(S)-hydroxypropyl]-N2-(pyridin-2-ylcarbonyl)-L-valinamide
项目整合开发状态: Biological Testing
项目研究机构: Medivir (Originator), Uppsala University (Originator)
合成路线:Coupling between epoxide (I) and amine (II) affords amino alcohol (III).The amino group of (III) is then protected with benzyl chloroformate to provide carbamate (IV).Removal of the N-Boc group of (IV) with trifluoroacetic acid yields amine (V),which is subsequently coupled with N-Boc-L-valine (VI) by means of TBTU to furnish amide (VII).After acidic Boc group cleavage in (VII),the resultant amine (VIII) is acylated by picolinic acid (IX) producing amide (X).
合成路线:The N-carbobenzoxy group of (X) is then removed by treatment with triflic acid,yielding (XI).Finally,Suzuki coupling of the aryl bromide (XI) with phenylboronic acid leads to the title biphenyl derivative.
📌 参考资料/链接:
参考文献标题:New antimalarials: Design and synthesis of protease inhibitors with effect in cultured parasite-infected human erythrocytes
文献作者:N鰐eberg,D.; et al.
参考来源:Drugs Fut 2002,27(Suppl.A),