CAS: 69-25-0; 23-(6-Amino-2-(3-Hydroxy-2-(1-(5-Oxopyrrolidine-2-Carbonyl)Pyrrolidine-2-Carboxamido)Propanamido)Hexanamido)-17-Benzyl-14-(Sec-Butyl)-5-Carbamoyl-8-Isobutyl-20-Methyl-7,10,13,16,19,22-Hexaoxo-2-Thia-6,9,12,15,18,21-Hexaazapentacosan-25-Oic Acid

(2S,3S)-2-Amino-3-Methyl-Pentanoic Acid {[(S)-1-((S)-1-Carbamoyl-3-Methylsulfanyl-Propylcarbamoyl)-3-Methyl-Butylcarbamoyl]-Methyl}-Amide,在 α-Chymotrypsin体系中,用 水 作为反应溶剂,以58%的收率获得产物依来多辛
参考文献:酶促肽片段缩合反应介质工程:Eledoisin和lh-Rh的合成.
标题:酶促肽片段缩合反应介质工程:Eledoisin和lh-Rh的合成.
摘要:研究了不同反应体系对α-胰凝乳蛋白酶催化从(7 + 4)和(5 + 5)片段合成eledoisin和lh-Rh肽的影响.在以下系统中确定肽的产量:缓冲水介质,冷冻溶液,有机介质和助溶剂混合物.量身定制的实验设置可以筛选一系列条件,使肽片段的消耗最少(2.1和2.5 Mm).在缓冲水溶液中获得最佳收率(eledoisin收率22%,Lh-Rh收率68%).发现缓冲液的选择对肽的产量有很大的影响.ph为9的硼酸硼酸和乙酸铵缓冲液提供了最佳结果.在缓冲的水性系统中,通过使用片段浓度(21和25 Mm)增加10倍来扩大两种合成的规模.在这些条件下,Eledoisin和lh-Rh的收率分别提高到57%和80%.此外,在合成eledoisin的过程中以及在硼酸硼酸缓冲液ph 9的存在下,肽从反应介质中沉淀出来,防止了二次水解,并促进了原位产物的纯化.
DOI:10.1016/s0968-0896(98)00046-7

专利信息

专利号:US-12351573-B2
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; CHENG KAI FAN
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2023159450-A1
优先权日:2020-05-08
标 题 :Dimers for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

专利号:US-11845970-B2
优先权日:2016-01-15
标 题:Endo-S2 mutants as glycosynthases, method of making and use for glycoengineering of glycoproteins
发明人：WANG LAI-XI; YANG QIANG; LI TIEZHENG; TONG XIN
权利人:UNIV MARYLAND
摘要:The present invention provides for recombinant Endo-S2 mutants (named Endo-S2 glycosynthases) that exhibit reduced hydrolysis activity and increased transglycosylation activity for the synthesis of glycoproteins wherein a desired sugar chain is added to a fucosylated or nonfucosylated GlcNAc-IgG acceptor. As such, the present invention allows for the synthesis and remodeling of therapeutic antibodies thereby providing for certain biological activities, such as, prolonged half-life time in vivo, less immunogenicity, enhanced in vivo activity, increased targeting ability, and/or ability to deliver a therapeutic agent.

专利号:US-5202235-A
优先权日:1986-08-18
标题 :Enzymatic method for the synthesis and separation of peptides
发明人：IACOBUCCI GUILLERMO A
权利人:COCA COLA CO
摘要:The present invention provides a method for the enzymatic synthesis of peptides accomplished by shifting the chemical equilibrium that exists in a reaction mixture between charged or ionized reacting amino acids and uncharged or non-ionized peptide product in the presence of a proteolytic enzyme such as thermolysin. The equilibrium is shifted by diffusion of the uncharged peptide product across an ion-rejection membrane which removes the uncharged peptide from the reaction mixture and preferably the diffused uncharged peptide is quickly converted to a charged species that cannot back-diffuse into the reaction mixture so that the uncharged peptide is effectively 'pulled' across the membrane.

专利号:US-5350681-A
优先权日:1986-08-18
标题 :Enzymatic membrane method for the synthesis and separation of peptides
发明人：IACOBUCCI GUILLERMO A; BROSE DANIEL J; RAY RODERICK J; VAN EIKEREN PAUL
权利人:COCA COLA CO
摘要:The present invention discloses a method for the enzymatic synthesis of a peptide. A protected peptide having a C-terminal carboxylate group or a protected, N-acyl amino acid having an alpha carboxylate group is reacted with a protected peptide having an N-terminal ammonium group or a protected amino acid having an alpha ammonium group in the presence of a condensation enzyme under conditions in which the carboxylate group and the ammonium group condense to form a protected, uncharged, peptide product. This peptide product is transported across a water-immiscible hydrophobic phase into an aqueous product phase and prevented from back diffusing across the water-immiscible hydrophobic phase. The peptide product can be converted, chemically or enzymatically, to a charged species that cannot back diffuse across the water-immiscible phase into the aqueous reaction phase. The water-immiscible hydrophobic phase is an ion rejection membrane separating the aqueous reaction phase from the product phase creating oil/water interfaces with each of the aqueous phases.