N-叔丁氧羰基-O-叔丁基-L-丝氨酸二环己胺盐置于硫酸体系中,用 水,乙酸乙酯 用作溶剂,化学反应生成N-叔丁氧羰基-O-叔丁基-L-丝氨酸 参考文献:Type 1,4-Naphtoquinone Compounds,Compositions Comprising Them And Use Of These Compounds As Anti-Cancer Agents 标题:Type 1,4-Naphtoquinone Compounds,Compositions Comprising Them And Use Of These Compounds As Anti-Cancer Agents 摘要:这项发明涉及以下给定的化合物(i)的公式或其药学上可接受的盐之一,作为药物;包含一个或多个具有公式(i)的化合物作为活性成分的药物组合物的公式(i),使用具有公式(i)的化合物制备旨在预防或治疗涉及异常细胞增殖的至少一种疾病的组合物,包含至少一种具有公式(i)的化合物的促凋亡组合物和/或抗增殖组合物,以及使用具有公式(i)的化合物作为促凋亡和/或抗增殖剂.
专利号:US-9388212-B2 优先权日:2013-02-21 标 题:Solid phase peptide synthesis via side chain attachment 发明人:BARLOS KLEOMENIS K 权利人:CHEMICAL & BIOPHARMACEUTICAL LAB OF PATRAS S A 摘要:The present application discloses peptides and peptaibols of high purity may be obtained by solid phase peptide synthesis using as the starting resin hydroxy amino acids, hydroxy amino acid amides, hydroxy amino alcohols or small peptides containing hydroxy amino acids attached to polymers through their side chain.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-11420997-B2 优先权日:2018-04-13 标题:Peptide synthesis method 发明人:SUZUKI HIDEAKI; MUTO SUSUMU; FUJITA SHUJI; KUBO DAISUKE 权利人:JITSUBO CO LTD 摘要:The present invention has an object of shortening the process time and reducing use of a poor solvent for solidifying a carrier (Tag)-peptide component, by removing impurities without conducting solid-liquid separation (condensation, solid-liquid separation and drying operation) of a Tag-peptide component, in an Fmoc method using a Tag for liquid phase peptide synthesis. Provided is the peptide synthesis method that includes the following steps a-d: step a: a carrier-protected amino acid, carrier-protected peptide, or a carrier-protected amino acid amide, and an N-Fmoc-protected amino acid or an N-Fmoc-protected peptide are condensed in an organic solvent or a mixed solution of organic solvents, to obtain an N-Fmoc-carrier-protected peptide, step b: a water-soluble amine is added to the reaction solution after the condensation reaction, step c: the Fmoc group is deprotected from the protected amino group in the presence of a water-soluble amine, and step d: the reaction solution is neutralized by adding an acid, and further, by adding and washing with an acidic aqueous solution, then, by liquid-liquid separation an aqueous layer is removed to obtain an organic layer.
专利号:US-8147799-B2 优先权日:2007-01-11 标题:Methods and compositions for improved F-18 labeling of proteins, peptides and other molecules 发明人:MCBRIDE WILLIAM J; GOLDENBERG DAVID M 权利人:MCBRIDE WILLIAM J; GOLDENBERG DAVID M; IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. In particular embodiments, the labeled molecules may be peptides or proteins, although other types of molecules including but not limited to aptamers, oligonucleotides and nucleic acids may be labeled and utilized for such imaging studies. In preferred embodiments, the F-18 label may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety, such as DOTA, NOTA, DTPA, TETA or NETA. In other embodiments, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other preferred embodiments, the F-18 labeled moiety may comprise a targetable conjugate that may be used in combination with a bispecific or multispecific antibody to target the F-18 to an antigen expressed on a cell or tissue associated with a disease, medical condition, or pathogen. Exemplary results show that F-18 labeled targetable conjugate peptides are stable in human serum at 37° C. for several hours, sufficient time to perform PET imaging analysis.
专利号:US-8153100-B2 优先权日:2007-01-11 标题 :Methods and compositions for F-18 labeling of proteins, peptides and other molecules 发明人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M 权利人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M; IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use of 18 F or 19 F labeled molecules of use in PET or MRI imaging. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled. Preferably, the 18 F or 19 F is conjugated to a targeting molecule by formation of a metal complex and binding of the 18 F- or 19 F-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the 18 F or 19 F bound to the metal. In other embodiments, the 18 F or 19 F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The 18 F or 19 F labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET or MRI imaging.
专利号:US-8147800-B2 优先权日:2007-01-11 标 题 :Methods and compositions for F-18 labeling of proteins, peptides and other molecules 发明人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M 权利人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M; IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled by the described methods. Preferably, the F-18 may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other embodiments, the F-18 labeled moiety may comprise a targetable construct used in combination with a bispecific or multispecific antibody to target F-18 to a disease-associated antigen, such as a tumor-associated antigen. The F-18 labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET imaging analysis.
参考标题:Convergent Synthesis Of Calcium-Dependent Antibiotic Cda3A And Analogues With Improved Antibacterial Activity Via Late-Stage Serine Ligation 作者:Delin Chen,Kathy Hiu Laam Po,Pilar Blasco,Sheng Chen,Xuechen Li |发布日期:2020.6.19 摘要:A Convergent Synthesis Via The Late-Stage Serine Ligation Of Naturally Occurring Calcium-Dependent Antibiotic Cda3A And Its Analogues Has Been Developed, Which Allowed Us To Readily Synthesize The Analogues With The Variation On The Lipid Tail. Some Analogues Were Found To Show 100-500-Fold Higher Antimicrobial Activity Than The Natural Compound Cda3A Against Drug Resistant Bacteria. This Study Will
合成参考文献
参考文献:10.1007/s00289-012-0733-y 摘要:Taniguchi I, Ootera Y, Chowdhury FA, Tomizaki K, Kai T, Kazama S. Polymeric membranes composed of polystyrenes tethering amino acids for preferential CO2 separation over H2. Polymer Bulletin. 2012 Mar 10;69(4):405–15. doi: 10.1007/s00289-012-0733-y.