77544-60-6 = 86770-67-4 反应条件:1.1 Reagents: Sodium Azide Solvents: Ethanol; 1 D,80 °C 标题:Zwitterion-Functionalized Detonation Nanodiamond With Superior Protein Repulsion And Colloidal Stability In Physiological Media 作者:Merz,Viktor; Et Al 参考文献:Small 日期:2019 卷标:15(48)]
77544-60-6 = 86770-67-4 反应条件:1.1 Reagents: Sodium Azide Solvents: Dimethylformamide; 8 H,70 °C 标题:Cell-Penetrating And Neurotargeting Dendritic Sirna Nanostructures 作者:Brunner,Korbinian; Et Al 参考文献:Angewandte Chemie 日期:2015 卷标:54(6) 页码:1946-1949]
1574267-61-0 = 86770-67-4 反应条件:1.1 Reagents: Sodium Azide Solvents: Dimethylformamide; 5 H,80 °C; 80 °C -> Rt1.2 Reagents: Sulfuric Acid Solvents: Tetrahydrofuran,Water; 1 H,Reflux1.3 Reagents: Sodium Bicarbonate Solvents: Water 标题:Amide Bond-Containing Monodisperse Polyethylene Glycols Beyond 10 000 Da 作者:Wan,Zihong; Et Al 参考文献:Organic & Biomolecular Chemistry 日期:2016 卷标:14(33) 页码:7912-7919]
1574267-56-3 = 86770-67-4 反应条件:1.1 Reagents: Sodium Periodate Catalysts: Ruthenium Trichloride Solvents: Carbon Tetrachloride,Acetonitrile,Water; 1 H,0 °C2.1 Reagents: Sodium Azide Solvents: Dimethylformamide; Overnight,Rt2.2 Catalysts: Amberlyst 15 Solvents: Tetrahydrofuran,Water; 12 H,Rt 标题:One-Pot Synthesis Of Monofunctionalized Oligoethylene Glycols Through Ring-Opening And Heterogeneous Hydrolysis Of Macrocyclic Sulfates 作者:Yang,Lan; Et Al 参考文献:Acs Omega 日期:2023 卷标:8(8) 页码:7684-7689]
25322-68-3 = 86770-67-4 反应条件:1.1 Reagents: Pyridine,Methanesulfonyl Chloride Solvents: Dichloromethane; 0 °C; 24 - 48 H,0 °C1.2 Reagents: Sodium Azide Solvents: Dimethylformamide; 16 - 72 H,80 °C 标题:Multivalent Thiosialosides And Their Synergistic Interaction With Pathogenic Sialidases 作者:Brissonnet,Yoan; Et Al 参考文献:Chemistry - A European Journal 日期:2019 卷标:25(9) 页码:2358-2365]
37860-51-8 + 77544-60-6 = 86770-67-4 反应条件:1.1 Reagents: Sodium Azide Solvents: Dimethylformamide; 24 H,60 °C 标题:Biomembrane Disruption By Silica-Core Nanoparticles: Effect Of Surface Functional Group Measured Using A Tethered Bilayer Lipid Membrane 作者:Liu,Ying; Et Al 参考文献:Biochimica Et Biophysica Acta 日期:2014 卷标:1838 页码:429-437]
112-60-7 + 104-15-4 = 86770-67-4 反应条件:1.1 Solvents: Pyridine; 6 H,Rt2.1 Reagents: Sodium Azide Solvents: Acetone,Water; Rt -> 60 °C; 12 H,60 °C2.2 Reagents: Sodium Carbonate Solvents: Water 标题:Discovery Of A New Class Of Protac Brd4 Degraders Based On A Dihydroquinazolinone Derivative And Lenalidomide/pomalidomide 作者:Zhang,Fangqing; Et Al 参考文献:Bioorganic & Medicinal Chemistry 日期:2020 卷标:28(1)]
112-60-7 + 10439-23-3 = 86770-67-4 反应条件:1.1 Reagents: Triethylamine Solvents: Dichloromethane; 0 °C; Overnight,Rt2.1 Reagents: Sodium Azide Solvents: Ethanol; 7 H,Reflux 标题:Synthesis Of Molecularly Encoded Oligomers Using A Chemoselective "Ab + Cd" Iterative Approach 作者:Trinh,Thanh Tam; Et Al 参考文献:Macromolecular Rapid Communications 日期:2014 卷标:35(2) 页码:141-145]
112-60-7 = 86770-67-4 反应条件:1.1 Reagents: Triethylamine,Sulfuryl Chloride Solvents: Tetrahydrofuran; Rt -> 0 °C; 0 °C; 0 °C -> Rt; Overnight,Rt2.1 Reagents: Sodium Azide Solvents: Ethanol; Overnight,Reflux; Reflux -> Rt 标题:Tailoring Carbon Nanotube Surfaces With Glyconanorings: New Bionanomaterials With Specific Lectin Affinity 作者:Khiar,Noureddine; Et Al 参考文献:Chemical Communications (Cambridge 日期:2009 卷标:(27) 页码:4121-4123]
65883-12-7 = 86770-67-4 反应条件:1.1 Reagents: Sodium Azide Solvents: Dimethylformamide 标题:Site-Specific And Covalent Attachment Of His-Tagged Proteins By Chelation Assisted Photoimmobilization: A Strategy For Microarraying Of Protein Ligands 作者:Ericsson,Emma M.; Et Al 参考文献:Langmuir 日期:2013 卷标:29(37) 页码:11687-11694]
65883-12-7 = 86770-67-4 反应条件:1.1 Reagents: Sodium Azide 标题:Membrane Activation: Selective Vesicle Fusion Via Small Molecule Recognition 作者:Gong,Yun; Et Al 参考文献:Journal Of The American Chemical Society 日期:2006 卷标:128(45) 页码:14430-14431]
65883-12-7 = 86770-67-4 反应条件:1.1 Reagents: Sodium Azide Solvents: Ethanol; Overnight,Reflux 标题:Glyconanosomes: Disk-Shaped Nanomaterials For The Water Solubilization And Delivery Of Hydrophobic Molecules 作者:Assali,Mohyeddin; Et Al 参考文献:Acs Nano 日期:2013 卷标:7(3) 页码:2145-2153]
134179-42-3 = 86770-67-4 反应条件:1.1 Reagents: Tetrabutylammonium Fluoride Solvents: Tetrahydrofuran; Overnight,Rt 标题:A Convergent Synthetic Platform For Single-Nanoparticle Combination Cancer Therapy: Ratiometric Loading And Controlled Release Of Cisplatin,Doxorubicin,And Camptothecin 作者:Liao,Longyan; Et Al 参考文献:Journal Of The American Chemical Society 日期:2014 卷标:136(16) 页码:5896-5899]
1574267-61-0 = 86770-67-4 反应条件:1.1 Reagents: Sodium Azide Solvents: Dimethylformamide; Overnight,Rt1.2 Catalysts: Amberlyst 15 Solvents: Tetrahydrofuran,Water; 12 H,Rt 标题:One-Pot Synthesis Of Monofunctionalized Oligoethylene Glycols Through Ring-Opening And Heterogeneous Hydrolysis Of Macrocyclic Sulfates 作者:Yang,Lan; Et Al 参考文献:Acs Omega 日期:2023 卷标:8(8) 页码:7684-7689]
1574267-61-0 = 86770-67-4 反应条件:1.1 Reagents: Sodium Azide Solvents: Dimethylformamide; Rt; 12 H,Rt1.2 Reagents: Sulfuric Acid Solvents: Tetrahydrofuran,Water; 1 H,Reflux1.3 Reagents: Sodium Bicarbonate Solvents: Water 标题:Highly Efficient Synthesis Of Monodisperse Poly(Ethylene Glycols) And Derivatives Through Macrocyclization Of Oligo(Ethylene Glycols) 作者:Zhang,Hua; Et Al 参考文献:Angewandte Chemie 日期:2015 卷标:54(12) 页码:3763-3767]
1574267-56-3 = 86770-67-4 反应条件:1.1 Reagents: Sodium Periodate Catalysts: Ruthenium Trichloride Solvents: Carbon Tetrachloride,Acetonitrile,Water; 0 °C; 1 H,0 °C2.1 Reagents: Sodium Azide Solvents: Dimethylformamide; Rt; 12 H,Rt2.2 Reagents: Sulfuric Acid Solvents: Tetrahydrofuran,Water; 1 H,Reflux2.3 Reagents: Sodium Bicarbonate Solvents: Water 标题:Highly Efficient Synthesis Of Monodisperse Poly(Ethylene Glycols) And Derivatives Through Macrocyclization Of Oligo(Ethylene Glycols) 作者:Zhang,Hua; Et Al 参考文献:Angewandte Chemie 日期:2015 卷标:54(12) 页码:3763-3767]
= 86770-67-4 反应条件:1.1 Reagents: Tetrabutylammonium Fluoride Solvents: Tetrahydrofuran; 0 °C; 12 H,Rt1.2 Reagents: Water; Rt 标题:Sialyltransferase Inhibitors Suppress Breast Cancer Metastasis 作者:Fu,Chih-Wei; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:2021 卷标:64(1) 页码:527-542]
112-60-7 = 86770-67-4 反应条件:1.1 Reagents: Tosyl Chloride,Sodium Hydroxide Solvents: Tetrahydrofuran,Water; 3 H,0 °C1.2 Reagents: Sodium Azide Solvents: Ethanol; Overnight,Reflux 标题:Modulation Of Coiled-Coil Binding Strength And Fusogenicity Through Peptide Stapling 作者:Crone,Niek S. A.; Et Al 参考文献:Bioconjugate Chemistry 日期:2020 卷标:31(3) 页码:834-843]
868594-38-1 = 86770-67-4 反应条件:1.1 Catalysts: P-Toluenesulfonic Acid Solvents: Methanol; Rt 标题:Synthesis And Ligation Ability Of Mono-Aminooxy-Functionalized Dendrigraft Poly-L-Lysine (Dgl) 作者:Bondia,Andrea Molero; Et Al 参考文献:Tetrahedron Letters 日期:2010 卷标:51(25) 页码:3330-3333]
86770-71-0 = 86770-67-4 反应条件:1.1 Reagents: Sodium Methoxide Solvents: Methanol; Rt; Overnight,Rt; Ph 7 标题:Towards A Universal Method For The Stable And Clean Functionalization Of Inert Perfluoropolymer Nanoparticles: Exploiting Photopolymerizable Amphiphilic Diacetylenes 作者:Morasso,Carlo; Et Al 参考文献:Advanced Functional Materials 日期:2010 卷标:20(22) 页码:3932-3940]
5197-66-0 = 86770-67-4 反应条件:1.1 Reagents: Ammonium Chloride,Sodium Azide Solvents: Water; Rt -> 80 °C 标题:Protein-Inorganic Array Construction: Design And Synthesis Of The Building Blocks 作者:Bogdan,Niculina D.; Et Al 参考文献:Chemistry - A European Journal 日期:2010 卷标:16(7) 页码:2170-2180]
155130-15-7 = 86770-67-4 反应条件:1.1 Reagents: Sodium Azide Solvents: Dimethylformamide,Water; Rt -> 60 °C; Overnight,60 °C 标题:Click Chemistry In Mesoporous Materials: Functionalization Of Porous Silicon Rugate Filters 作者:Ciampi,Simone; Et Al 参考文献:Langmuir 日期:2008 卷标:24(11) 页码:5888-5892]
1253389-31-9 = 86770-67-4 反应条件:1.1 Reagents: 4-[bis(1,1-Dimethylethyl)Phosphino]-N,N-Dimethylbenzenamine Solvents: Tetrahydrofuran; 1 H,Rt1.2 Reagents: Lithium Aluminum Hydride Solvents: Tetrahydrofuran; 3 H,Rt1.3 Reagents: Ammonium Chloride Solvents: Water; Rt1.4 Reagents: S8 Solvents: Tetrahydrofuran; 24 H,Rt 标题:Nucleophilic Transformations Of Azido-Containing Carbonyl Compounds Via Protection Of The Azido Group 作者:Aimi,Takahiro; Et Al 参考文献:Chemical Communications (Cambridge 日期:2021 卷标:57(49) 页码:6062-6065]
86770-74-3 = 86770-67-4 反应条件:1.1 Reagents: Potassium Bicarbonate,Sulfuryl Azide Fluoride Solvents: Dimethylformamide,Tert-Butyl Methyl Ether,Water; 5 Min,Rt1.2 Reagents: Hydrochloric Acid Solvents: Water; Acidified,Rt 标题:Modular Click Chemistry Libraries For Functional Screens Using A Diazotizing Reagent 作者:Meng,Genyi; Et Al 参考文献:Nature (London 日期:2019 卷标:574(7776) 页码:86-89]
= 86770-67-4 反应条件:1.1 Reagents: Sodium Azide Solvents: Ethanol; 16 H,Rt -> Reflux2.1 Reagents: Tetrabutylammonium Fluoride Solvents: Tetrahydrofuran; 0 °C; 12 H,Rt2.2 Reagents: Water; Rt 标题:Sialyltransferase Inhibitors Suppress Breast Cancer Metastasis 作者:Fu,Chih-Wei; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:2021 卷标:64(1) 页码:527-542]
112-60-7 + 104-15-4 = 86770-67-4 反应条件:1.1 Reagents: Sodium Hydroxide Solvents: Tetrahydrofuran,Water; Rt -> 0 °C1.2 Solvents: Tetrahydrofuran; 2 H,0 °C; 3 H,0 °C2.1 Reagents: Sodium Azide Solvents: Dimethylformamide; 5 H,60 °C 标题:Towards Potential Nanoparticle Contrast Agents: Synthesis Of New Functionalized Peg Bisphosphonates 作者:Kachbi-Khelfallah,Souad; Et Al 参考文献:Beilstein Journal Of Organic Chemistry 日期:2016 卷标:12 页码:1366-1371
13,13,14,14-四甲基-3,6,9,12-四氧杂-13-硅-1-十五醇置于sodium Azide,四丁基氟化铵,三乙胺体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 26.0H,反应生成 11-叠氮基-3,6,9-三氧杂十一醇 参考文献: Inhibitors Of Hepatitis C Virus Polymerase[fr] Inhibiteurs De Polymérase Du Virus De L'Hépatite C 标题: Inhibitors Of Hepatitis C Virus Polymerase[fr] Inhibiteurs De Polymérase Du Virus De L'Hépatite C 摘要:本发明提供了一种由一般式i表示的化合物,以及其药学上可接受的盐,其中l和a(以及进一步的取代基)如本文中的类和子类中所定义,并且包括这些化合物的组合物(例如,药物组合物),这些化合物可用作丙型肝炎病毒聚合酶的抑制剂,因此可用作治疗hcv感染的药物.
专利号:US-5135737-A 优先权日:1986-11-10 标 题:Amplifier molecules for enhancement of diagnosis and therapy 发明人:KEANA JOHN F W 权利人:OREGON STATE 摘要:Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
专利号:WO-9403593-A1 优先权日:1992-08-04 标题 :Amplifier molecules for enhancement of diagnosis and therapy 发明人:KEANA JOHN F W 权利人:OREGON STATE 摘要:Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
专利号:US-5412148-A 优先权日:1986-11-10 标题:Amplifier molecules derived from diethylene triaminepentaacetic acid for enhancement of diagnosis and therapy 发明人:KEANA JOHN F W 权利人:OREGON STATE 摘要:Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
专利号:US-7799524-B2 优先权日:2002-10-03 标 题:Substrates for O6-alkylguanina-DNA alkyltransferase 发明人:KINDERMANN MAIK; JOHNSSON KAI; BIERI CHRISTOPH 权利人:ECOLE POLYTECHNIQUE FERDEALE D 摘要:The invention relates to compounds of formula 1 n nwherein R 1 -R 2 is a guanine derivative; X is oxygen or sulfur; R 3 is a heteroaromatic, unsaturated heterocyclyl or an alkynyl group with the double or triple bond connected to CH 2 ; R 4 is a linker; and L is a label, a plurality of same or different labels, a bond connecting R 4 to R 1 forming a cyclic substrate, or a further group —R 3 —CH 2 —X—R 1 -R 2 . The invention relates also to methods of manufacture of such novel AGT substrates, to intermediates useful in the synthesis of such AGT substrates, and to a method of transferring a label from such AGT substrates to O 6 -alkylguanine-DNA alkyltransferase (AGT) fusion proteins comprising proteins of interest.
专利号:US-8076496-B2 优先权日:2000-03-16 标题:Chemoselective ligation 发明人:SAXON ELIANA; BERTOZZI CAROLYN RUTH 权利人:SAXON ELIANA; BERTOZZI CAROLYN RUTH; UNIV CALIFORNIA 摘要:The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
1: Brown A, Patel S, Ward C, Lorenz A, Ortiz M, DuRoss A, Wieghardt F, Esch A, Otten EG, Heiser LM, Korolchuk VI, Sun C, Sarkar S, Sahay G. PEG-lipid micelles enable cholesterol efflux in Niemann-Pick Type C1 disease-based lysosomal storage disorder. Sci Rep. 2016 Aug 30;6:31750. doi: 10.1038/srep31750. 2: Saifer MG, Williams LD, Sobczyk MA, Michaels SJ, Sherman MR. Selectivity of binding of PEGs and PEG-like oligomers to anti-PEG antibodies induced by methoxyPEG-proteins. Mol Immunol. 2014 Feb;57(2):236-46. doi: 10.1016/j.molimm.2013.07.014. Epub 2013 Nov 5. doi: 10.1517/17425247.2012.720969. Epub 2012 Aug 30.
合成参考文献
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