60-32-2 + 82911-69-1 = 88574-06-5 反应条件:1.1 Reagents: Sodium Bicarbonate Solvents: 1,4-Dioxane,Water; 16 H,Rt 标题:A Pendant Peptide Endows A Sunscreen With Water-Resistance 作者:Ellison,Aubrey J.; Raines,Ronald T. 参考文献:Organic & Biomolecular Chemistry 日期:2018 卷标:16(39) 页码:7139-7142
(9H-芴-9-基)甲基 2,5-二氧代吡咯烷-1-羧酸,6-氨基己酸置于碳酸氢钠体系中,用 水,丙酮 作为反应溶剂,化学反应 3.0H,以99%的收率获得产物芴甲氧羰酰基-6-氨基己酸 参考文献: 标题: 摘要:The Thioamide Derivatives 3'-Deoxy-5'-O-(4,4'-Dimethoxytrityl)-3'-[(2-Methyl-1-Thioxopropyl)Amino] Thymidine (4A) And 3'-Deoxy-5'-O-(4,4'-Dimethoxytrityl)-3'-{{6-{[9H-(Fluoren-9-Ylmethoxy)Carbonyl]Amino}-1-Thioxohexyl}Amino}Thymidine (4B) Were Synthesized By Regioselective Thionation Of The Corresponding Amides 3A And 3B With 2,4-Bis(4-Methoxyphenyl)-1,3,2,4-Dithiadiphosphetane 2,4-Disulfide (Lawesson'S Reagent). The Addition Of Exact Amounts Of Pyridine To The Reaction Mixture Proved To Be Essential For An Efficient Transformation. The Thioamides Were Converted Into The Corresponding 5'-Triphosphates 6A And 6B. Compound 6A Was Chosen For Dna Sequencing Experiments,And 6B Was Further Labelled With Fluorescein (-->8). DOI:10.1002/1522-2675(20000607)83:6<1268::Aid-Hlca1268>3.0.Co;2-S
专利号:US-2024018099-A1 优先权日:2020-11-19 标题 :Synthesis of prostate specific membrane antigen (psma) ligands 发明人:ANDREAE FRITZ 权利人:NOVARTIS AG 摘要:The present disclosure relates to the synthesis of prostate specific membrane antigen (PSMA) ligands that are useful in the treatment of diseases like cancer. In particular, the disclosure relates to a method for synthesizing PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal.
专利号:US-2023272006-A1 优先权日:2021-08-31 标题:Peptidomimetics and method of synthesis thereof 发明人:NEFZI ADEL 权利人:NEFZI ADEL; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides compounds, peptidomimetics, and methods of synthesis thereof. The subject invention provides the synthesis and use of guanidino acids and/or poly guanidino acids not only as vehicles for drug delivery but as toolbox for drug discovery. The peptidomimetic of the subject invention comprises oligo(guanidino acid)s or poly(guanidino acid)s with guanidines as peptide bond surrogates. The incorporation of the guanidine as amide bond surrogates offers significant differences in polarity, hydrogen bonding capability, and acid-base character.
专利号:US-8853132-B2 优先权日:2008-11-27 标题 :Directed synthesis of oligophosphoramidate stereoisomers 发明人:HEINDL DIETER; KESSLER DIRK; ROESLER ANGELIKA; SEIDEL CHRISTOPH; THUER WILMA 权利人:ROCHE DIAGNOSTICS OPERATIONS 摘要:The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.
专利号:WO-02076965-A1 优先权日:2001-03-23 标 题 :Non peptide mimetics based on the active sequence s42fllr46 of the thrombin receptor for the treatment of thrombosis and cancer 发明人:MATSOUKAS JOHN; MARAGOUDAKIS MICHAEL; VLAHAKOS DEMETRIOS; ALEXOPOULOS KOSTAS 权利人:MATSOUKAS JOHN; MARAGOUDAKIS MICHAEL; VLAHAKOS DEMETRIOS; ALEXOPOULOS KOSTAS 摘要:The invention relates to novel non peptide compounds (mimetics) based on a thrombin receptor sequence and novel methods for the synthesis of these compounds. These compounds act as agonists or antagonists in a variety of cells including endothelial cells, blood platelets, vascular smooth muscle cells and tumor cells. They are useful in the treatment of thrombosis an cardiovascular diseases and modulation of angiogenesis for cancer treatment or wound healing.
专利号:US-5726243-A 优先权日:1993-06-30 标题 :Mild solid-phase synthesis of aligned, branched triple-helical peptides 发明人:FIELDS GREGG B 权利人:UNIV MINNESOTA 摘要:A triple-helical polypeptide of the formula: ##STR1## is provided wherein: Z is Hyp or Pro; each X and Y is an amino acid such that (Gly-X-Y) m is a sequence of a collagen cell adhesion site; said X and Y may be the same or different and each (Gly-X-Y) may be the same or different; O is an amino acid having a single side-chain amino group; J is an amino acid capable of acting as a chromophore; U is an amino acid; u=0 or 1; n≦30; m≦30; m+n≦30; and j≧1. Methods of making these compounds and intermediates used in the methods, are also provided.
专利号:US-2010056392-A1 优先权日:2005-06-15 标题:Microstructure and microdomain microarrays, methods of making same and uses thereof 发明人:GREVING MATTHEW; WOODBURY NEAL; NORTHEN TRENT R 权利人:GREVING MATTHEW; WOODBURY NEAL; NORTHEN TRENT R 摘要:Disclosed are methods for direct characterization of microdomains and/or three-dimensional microstructure arrays bearing high densities of reactive sites using Matrix Assisted Laser Desorption Ionization Time of Flight Mass Spectrometery (MALDI-MS) and other analytical techniques. The high site density of the arrays can provide sufficient sample of each array element and/or materials bound to each element to obtain directly using common analytical techniques such as MALDI-MS. Spatially directed synthesis of heteropolymers is done through the use of pliotolabile, electrically labile, and chemically labile protecting group(s).
参考文献:10.1007/s00706-024-03227-y 摘要:Dorn T, Finšgar M, Stana Kleinschek K, Steindorfer T, Thonhofer M, Wrodnigg TM, Kargl R. Covalent modification of chitosan surfaces with a sugar amino acid and lysine analogues. Monatsh Chem. 2024 Aug 03;156(1):65–75. doi: 10.1007/s00706-024-03227-y. 参考文献:10.1007/s10989-025-10752-9 摘要:Khan KR, Niedrauer ML, Hostetler MA, Kang SS, Lipton MA. A Photolabile Backbone Amide Linker for the Solid-Phase Synthesis of Cyclic Peptides and C-terminal Thioesters. Int J Pept Res Ther. 2025 Sep 08;31(5). doi: 10.1007/s10989-025-10752-9.