Synthesis of VIP-lipopeptide using a new linker to modify liposomes: towards the development of a drug delivery system for active targeting.
Synthesis of VIP-lipopeptide using a new linker to modify liposomes: towards the development of a drug delivery system for active targeting.
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DOI：
10.1248/cpb.c13-00518
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发表时间：
2013-11
影响因子：
1.7
通讯作者：
T. Masaka;T. Matsuda;Yingpeng Li;Yukiye Koide;Akira Takami;Kenji Yano;Ryosuke Imai;Risa Ichihara;N. Yagi;Hideharu Suzuki;Hidemasa Hikawa;K. Terada;Y. Yokoyama
中科院分区：
文献类型：
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作者：
T. Masaka;T. Matsuda;Yingpeng Li;Yukiye Koide;Akira Takami;Kenji Yano;Ryosuke Imai;Risa Ichihara;N. Yagi;Hideharu Suzuki;Hidemasa Hikawa;K. Terada;Y. Yokoyama
以(-)-2,3- o -异丙基-d -苏糖醇(3)为原料，设计了2-[(4R,5R)-5-（{（9h -芴-9-基）甲氧基]羰基氨基甲基}-2,2-二甲基-1,3-二氧基-4-基）甲氧基]乙酸(2)的固相合成新组分。关键步骤是在Cs2CO3存在下，3与溴乙酸苄酯选择性烷基化。采用固相肽合成方法合成了含有该连接体的血管活性肠肽(VIP)-脂肽(1)。
A new component for the solid phase peptide synthesis of lipopeptide, 2-[(4R,5R)-5-({[(9H-fluoren-9-yl)methoxy]carbonylaminomethyl}-2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]acetic acid (2), was designed and synthesized from (-)-2,3-O-isopropylidene-D-threitol (3) in 4 steps. The key step was the selective alkylation of 3 with benzyl bromoacetate in the presence of Cs2CO3. Vasoactive intestinal peptide (VIP)-lipopeptide (1) incorporating this linker was synthesized by solid phase peptide synthesis.