N-羟基-5-降冰片烯-2,3-二甲酰亚胺置于吡啶,Sodium Hydroxide,Tertiary Amine体系中,用 1,4-二氧六环,水 作为反应溶剂,化学反应 9.0H,反应生成 Fmoc-L-天冬氨酸 Beta-叔丁酯 参考文献:5-Norbornene-2,3-Dicarboximido Carbonochloridate. A New Stable Reagent For The Introduction Of Amino-Protecting Groups 标题:5-Norbornene-2,3-Dicarboximido Carbonochloridate. A New Stable Reagent For The Introduction Of Amino-Protecting Groups 摘要:报道了一种基于n-羟基-5-降冰片烯-2,3-二羧亚胺衍生的新碳酰氯化物的活化碳酸盐的合成.这些活化碳酸酯是引入目前所有使用的氨基甲酸酯保护基团的优秀试剂. DOI:10.1055/s-1987-27873
专利号:US-2008287649-A1 优先权日:2006-12-29 标 题 :Methods for the synthesis of cyclic peptides 发明人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 摘要:Methods for the synthesis of cyclic peptides are provided, as well as novel dipeptide compounds. The methods include the solid phase synthesis of a dipeptide, which is the coupled to a second peptide in a solid phase reaction. The peptide is then cyclized following the coupling reaction. The methods and dipeptides are particularly useful for the synthesis of MC-4 receptor agonist peptides.
专利号:US-2013267680-A1 优先权日:2010-09-15 标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof 发明人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL 权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST 摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.
专利号:US-2023242581-A1 优先权日:2020-06-17 标题:Synthesis of a guanylate cyclase agonist by fragments based approach 发明人:SAMBASIVAM GANESH; KASTURCHAND GODHA ATUL; VENKATA BHAGYARAJ ARETI; ANNADURAI SATHYA; VEERANJANEYULU AVULA; VASANTRAO GADAKH AMOL; S JADHAV DIPAK 权利人:ANTHEM BIOSCIENCES PRIVATE LTD 摘要:The present invention provides a process for the synthesis of Plecanatide, a guanylate cyclase agonist. The process involves convergent synthesis with compounds, i.e., fragment of peptides followed by cyclization. The method provides high yield of Plecanatide with less impurities.
专利号:US-5817751-A 优先权日:1994-06-23 标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives 发明人:SZARDENINGS ANNA KATRIN; CAMPBELL DAVID 权利人:AFFYMAX TECH NV 摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
专利号:US-2024067694-A1 优先权日:2021-01-04 标 题:Synthesis of teduglutide 发明人:GANGA RAMU VASANTHAKUMAR; PATIL NITIN; SUVARNA DEEPA SHANKAR 权利人:BIOCON LTD 摘要:The present invention provides for novel synthetic approach of solid phase synthesis of peptides with C-terminal Aspartic acid by anchoring the side chain carboxylic group of aspartic acid to the solid support to avoid the formation of various impurities and thus resulting in higher yield and ease the purification process. The present invention further provides the usage of free amino acids and reducing agents as antioxidants in the cleavage cocktail to negate the formation of oxidative impurities formed during the global cleavage and isolation of the peptide from solid support.
专利号:US-6316593-B1 优先权日:1996-02-09 标题:Synthesis of VIP analog 发明人:BOLIN DAVID ROBERT; DANHO WALEED; FELIX ARTHUR M 权利人:HOFFMANN LA ROCHE 摘要:This invention relates to a novel process for the synthesis of vasoactive intestinal peptide analog Ac(1-31)-NH2 from four protected peptide fragments.
[参考文献]: Esquivel J B, Et Al. Chiral Hplc Separation Of Protected Amino Acids. Journal Of Liquid Chromatography & Related Technologies, 1998, 21(6): 777-791. [参考文献]: Charity Wayua, Et Al. Evaluation Of A Nonpeptidic Ligand For Imaging Of Cholecystokinin 2 Receptor-Expressing Cancers. J Nucl Med. 2015 Jan;56(1):113-9.
合成参考文献
摘要:Graham, J. S.; Stanway-Gordon, H. A.; Waring, M. J., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 431.