新产品编号:288433
Chemical Name: Octadecanoyl-L-lysyl-L-lysyl-L-tyrosyl-L-leucinamide
CAS No. 197907-73-6
项目整合开发状态: Preclinical
项目研究机构: Yeda (Originator)
合成路线: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: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.
📌 参考资料/链接：
参考文献标题:Conjugates of lipophilic moieties and fragments of vasoactive intestinal peptide (VIP)
文献作者:Gozes,I.; Fridkin,M.(Yeda Research & Development Co.Ltd.)
参考来源:WO 9740070
📄 详细内容
合成路线: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: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.
参考文献标题:Mapping the active site in vasoactive intestinal to a core of four amino acids: Neuroprotective drug design
文献作者:Gozes,I.; Perl,O.; Giladi,E.; Davidson,A.; Ashur-Fabian,O.; Rubinraut,S.; Fridkin,M.
参考来源:Proc Natl Acad Sci USA 1999,96(7),4143