2-((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)-3-(Pyridin-3-yl)Propanoic Acid置于ammonium Hydroxide,三甲基氯硅烷,α-Chymotrypsine,Ammonium Acetate体系中,用 水,N,N-二甲基甲酰胺 用作溶剂,化学反应 38.0H,反应生成Methyl (R)-2-((((9H-Fluoren-9-yl)Methoxy)Carbonyl)Amino)-3-(Pyridin-3-yl)Propanoate,Fmoc-3-(3-吡啶基)-L-丙氨酸 参考文献:Chemoenzymatic Routes To Enantiomerically Pure 2-Azatyrosine And 2-,3-And 4-Pyridylalanine Derivatives 标题:Chemoenzymatic Routes To Enantiomerically Pure 2-Azatyrosine And 2-,3-And 4-Pyridylalanine Derivatives 摘要:Enantiomerically Pure 2-,3-Or 4-Pyridylalanine (Pya) And 2-Azatyrosine (Azatyr) Are Known To Present Various Biological Activities. After Incorporation Into Appropriate Peptide Sequences,These Heterocyclic Non Natural Alpha-Amino Acids Could Behave As New Substrates Or Inhibitors Of Elastase From Pseudomonas Aeruginosa. This Enzyme Is Known To Be Involved In Nosocomial Infections And Infections Related To The Cystic Fibrosis Disease. New Efficient Chemoenzymatic Preparations Of Those Compounds Using Alpha-Chymotrypsin (Alpha-Ct) Are Presented. Doi:10.1007/s00726-010-0829-3
专利号:US-2023391818-A1 优先权日:2020-11-05 标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation 发明人:NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.
专利号:WO-2023214577-A1 优先权日:2022-05-02 标 题 :Peptide synthesis method for suppressing defect caused by diketopiperazine formation 发明人:KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO; NOMURA KENICHI 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:The present invention addresses the problem of a desired elongation reaction not progressing as a result of a 6-membered cyclic amidine skeleton structure and a diketopiperazine formed when removing an N-terminated protective group during peptide synthesis. The inventors have discovered that it is possible to solve said problem during peptide production by treating a peptide protected by an N-terminated amino group in a protective group having an Fmoc skeleton by using a base which has a pKa of 23 or higher in an acetonitrile of a conjugate acid in a specific solvent, and next, performing peptide chain elongation.
专利号:US-8338565-B2 优先权日:2008-08-20 标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha 发明人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P 权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP 摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.
专利号:WO-2022265577-A2 优先权日:2021-06-15 标题:Coronavirus enzyme modulators, methods of synthesis and uses thereof