【药物名称】GS-2888
化学结构式(Chemical Structure):
参考文献No.32810
标题:Cationic lipids for delivery of nucleic acids to cells
作者:Deprince, R.B.; Facchine, K.L.; Lewis, G.S.; Lewis, J.G.; Lin, K.-Y.; Matteucci, M.D.; Mook, R.A. Jr.; Wagner, R.W. (Gilead Sciences Inc.; Glaxo Wellcome plc)
来源:WO 9601841
合成路线图解说明:

Benzyloxycarbonylglycine (I) was coupled with N-hydroxysuccinimide in the presence of dicyclohexylcarbodiimide (DCC), and the resulting succinimidyl active ester (II) was condensed with dimiristylamine (III) to afford amide (IV). The benzyloxycarbonyl group was then removed by hydrogenolysis in the presence of palladium on carbon to yield amine (V). Coupling of this amine with Boc-protected L-arginine (VI) in the presence of diisopropylcarbodiimide (DIC) gave dipeptide (VII). Finally, partial deprotection of Boc groups with hydrochloric acid in dioxane provided the title compound.

参考文献No.400577
标题:A serum-resistant cytofectin for cellular delivery of antisense oligodeoxynucleotides and plasmid DNA
作者:Lewis, J.G.; et al.
来源:Proc Natl Acad Sci USA 1996,93(8),3177
合成路线图解说明:

Benzyloxycarbonylglycine (I) was coupled with N-hydroxysuccinimide in the presence of dicyclohexylcarbodiimide (DCC), and the resulting succinimidyl active ester (II) was condensed with dimiristylamine (III) to afford amide (IV). The benzyloxycarbonyl group was then removed by hydrogenolysis in the presence of palladium on carbon to yield amine (V). Coupling of this amine with Boc-protected L-arginine (VI) in the presence of diisopropylcarbodiimide (DIC) gave dipeptide (VII). Finally, partial deprotection of Boc groups with hydrochloric acid in dioxane provided the title compound.

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