📜2-氮杂环壬酮置于sodium Hydroxide体系中,用 1,4-二氧六环,水 作为反应溶剂,化学反应 5.25H,反应生成 Boc-8-氨基辛酸 参考文献:A Practical Synthesis Of ω-Aminoalkanoic Acid Derivatives From Cycloalkanones 标题:A Practical Synthesis Of ω-Aminoalkanoic Acid Derivatives From Cycloalkanones 摘要:A Practical Synthetic Route To N-Boc Protected Or Boc-Amino Acid Coupled Omega-Aminoalkanoic Acids Is Reported And Exemplified By The Preparation Of 8-(T-Butoxycarbonylamino)Caprylic Acid 2 And (N-T-Butoxycarbonylphenylalanyl)-8-Aminocaprylic Acid 3. The Sequence Does Not Involve Column Chromatography,Hydrogenation,Azide Or Bromine Related Rearrangements,And Therefore Is Amenable To Scale-Up. Homologues Of The Omega-Aminoalkanoic Acid Derivatives May Also Be Prepared By Using Different Cycloalkanones. DOI:10.1080/00397919608004580
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-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
专利号:US-5175146-A 优先权日:1989-12-05 标题 :Synthetic calcitonin peptides 发明人:BASAVA CHANNA; HOSTETLER KARL Y 权利人:VICAL INC 摘要:Synthetic hypocalcemic peptides which are similar in biological properties to native calcitonins as clinically useful agents. The peptides comprise analogues of native calcitonins having amino acid substitutions and deletions which act to improve potency, prolong duration of the hormonal effect, enhance receptor binding, and increase oral or nasal bioavailability. The calcitonin peptide analogues are less expensive and more easily synthesized than native calcitonins, and have improved resistance to inactivation or degradation. Methods are provided for the synthesis of these peptides. Also, disclosed are novel cyclic peptides, including calcitonin, having increased stability with respect to proteolysis. Methods for the synthesis of these peptides are provided, comprising converting disulfide cyclic peptides and proteins to enzymatically and chemically stable cyclic peptide structures by the replacement of cysteine residues with dicarboxylic acids and diamino acids. The method is applicable to various naturally occurring peptides, their synthetic analogues or derivatives, and proteins.
专利号:US-2021002217-A1 优先权日:2013-11-18 标题:Method of synthesis of an ionizable cationic lipid
专利号:RU-2586931-C2 优先权日:2012-02-28 标 题 :Hyaluronic acid derivatives capable of forming hydrogels, synthesis method thereof, hydrogels based on said derivatives, method for production and use thereof
专利号:NZ-505979-A 优先权日:1998-06-08 标 题 :Multibinding antibacterial agents comprising 2 antibiotic or aglycone ligands, connected by a linker, capable of affecting cell wall synthesis or metabolism
[参考文献]: B J Bradbury, Et Al. Functionalized Congener Approach For The Design Of Novel Muscarinic Agents. Synthesis And Pharmacological Evaluation Of N-Methyl-N-[4-(1-Pyrrolidinyl)-2-Butynyl] Amides. J Med Chem. 1990 Feb;33(2):741-8.
合成参考文献
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