【药物名称】
化学结构式(Chemical Structure):
参考文献No.39395
标题:Conjugates of lipophilic moieties and fragments of vasoactive intestinal peptide (VIP)
作者:Gozes, I.; Fridkin, M. (Yeda Research & Development Co. Ltd.)
来源:WO 9740070
合成路线图解说明:

The solid-phase method of peptide synthesis, with an ABIMED AMS 422 synthesizer and a Rink amide resin have been used. N-Fmoc-L-Leucine (I) was attached to Rink amide resin using benzotriazol-1-yloxytripyrrolidinophosphonium hexafluorophosphate as the coupling reagent, and the Fmoc protecting group was subsequently removed to afford resin (II). Further coupling and deprotection cycles with N-Fmoc-L-tyrosine(O-t--Bu) (III), N-Fmoc-N-Boc-L-lysine (V) and again N-Fmoc-N-Boc-L-lysine (V) provided peptide resins (IV), (VI) and (VII), respectively.

合成路线图解说明:

Peptide resin (VII) was then coupled with stearic acid to yield (VIII). Finally, the target peptide amide was deprotected and cleaved from the resin by means of a mixture of trifluoroacetic acid, water and triethylsilane.

参考文献No.533672
标题:Mapping the active site in vasoactive intestinal to a core of four amino acids: Neuroprotective drug design
作者:Gozes, I.; Perl, O.; Giladi, E.; Davidson, A.; Ashur-Fabian, O.; Rubinraut, S.; Fridkin, M.
来源:Proc Natl Acad Sci USA 1999,96(7),4143
合成路线图解说明:

The solid-phase method of peptide synthesis, with an ABIMED AMS 422 synthesizer and a Rink amide resin have been used. N-Fmoc-L-Leucine (I) was attached to Rink amide resin using benzotriazol-1-yloxytripyrrolidinophosphonium hexafluorophosphate as the coupling reagent, and the Fmoc protecting group was subsequently removed to afford resin (II). Further coupling and deprotection cycles with N-Fmoc-L-tyrosine(O-t--Bu) (III), N-Fmoc-N-Boc-L-lysine (V) and again N-Fmoc-N-Boc-L-lysine (V) provided peptide resins (IV), (VI) and (VII), respectively.

合成路线图解说明:

Peptide resin (VII) was then coupled with stearic acid to yield (VIII). Finally, the target peptide amide was deprotected and cleaved from the resin by means of a mixture of trifluoroacetic acid, water and triethylsilane.

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