Z-L-天冬酰胺叔丁酯置于palladium-Carbon 氢气,甲醇体系中,用 乙酸乙酯 用作溶剂,化学反应 1.0H,反应生成L-天冬酰胺叔丁酯 参考文献:Process For The Manufacture Of Cystine-Containing Peptides 标题:Process For The Manufacture Of Cystine-Containing Peptides 摘要:本发明涉及一种改进的方法,用于从含有s-三苯基甲基保护基的半胱氨酸氨基酸序列中制备含半胱氨酸的肽,其中s-三苯基甲基半胱氨酸序列直接与碘氧化以产生半胱氨酸二硫键.
专利号:WO-9849186-A1 优先权日:1997-04-25 标 题:Dipeptide surrogates containing asparagine-derived tetrahydropyrimidinones 发明人:KONOPELSKI JOSEPH P; FILONOVA LUBOV K 权利人:UNIV CALIFORNIA 摘要:Dipeptide surrogates Fmoc-Xxx-(cyclo)Asn-OBu are prepared from asparagine, aromatic aldehydes, and Fmoc-protected amino acid chlorides. The tetrahydropyrimidinone structure exist in a preferred ring conformation, as observed in a single crystal X-ray analysis of one of the derived carboxylic acids. As with other molecules with similar substitution patterns, the six-membered ring is held in a boat conformation. These dipeptide building blocks are deprotected at the C-terminal and/or N-terminal positions by known protocols. In addition, they function as ready participants for solid phase peptide synthesis. Finally, the constrained asparagine residue can be transformed to the native amino acid within a polypeptide framework, allowing for the direct interchange of a restricted system of known conformation and configuration to the native state under mild conditions. These peptide surrogates containing (cyclo)Asn are useful therapy of mammalian disease conditions, particularly in therapy of brain disorders.
参考标题:Allenone-Mediated Racemization/epimerization-Free Peptide Bond Formation And Its Application In Peptide Synthesis 作者:Zhengning Wang,Xuewei Wang,Penghui Wang,Junfeng Zhao |发布日期:2021.7.14 摘要:Peptide Synthesis (Spps). The Robustness Of The Allenone-Mediated Peptide Bond Formation Was Showcased Incisively By The Synthesis Of Carfilzomib, Which Involved A Rare Racemization-/epimerization-Free N To C Peptide Elongation Strategy. Furthermore, The Successful Synthesis Of The Model Difficult Peptide Acp (65-74) On A Solid Support Suggested That This Method Was Compatible With Spps. This Method Combines
合成参考文献
摘要:Sasano, Y.; Iwabuchi, Y., Science of Synthesis: Special Topics, (2022) 1, 345.