3-硝基苯硼酸频哪醇酯置于盐酸,Polystyrene Boronic Acid体系中,用 乙腈 用作溶剂,化学反应 18.0H,以88%的收率获得3-硝基苯硼酸 参考文献:Deprotection Of Pinacolyl Boronate Esters By Transesterification With Polystyrene-boronic Acid 标题:Deprotection Of Pinacolyl Boronate Esters By Transesterification With Polystyrene-boronic Acid 摘要:Mild Deprotection Of Pinacolyl Boronate Esters To The Corresponding Boronic Acids Was Achieved In The Presence Of Excess Polystyrene-Boronic Acid Via A Transesterification Process. The Procedure Allows For The Cleavage Of Pinacolyl Boronate Esters In The Presence Of Sensitive Functional Groups. Crown Copyright (C) 2004 Published By Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Tetlet.2004.07.014
专利信息
专利号:WO-2013057110-A1 优先权日:2011-10-19 标 题:Method for the synthesis of citric acid esters 发明人:ALTENBACH HANS-JOSEF; LANGE KARSTEN; NANDI SUKHENDU; IHIZANE RACHID; JAKOB BERND; SCHNEIDER MANFRED 权利人:BERGISCHE UNI WUPPERTAL; ALTENBACH HANS-JOSEF; LANGE KARSTEN; NANDI SUKHENDU; IHIZANE RACHID; JAKOB BERND; SCHNEIDER MANFRED 摘要:The present invention discloses a targeted synthesis method for the synthesis of asymmetric monoesters and/or symmetrical diesters of citric acid through acidic esterification by using boric acid or a boronic acid as a catalyst. The boric/boronic acid simultaneously acts as a catalyst, as well as a 'protecting group' for the tertiary carboxylic acid, and therefore specifically only the asymmetric monoesters or symmetrical diesters are created.
专利号:US-11738092-B2 优先权日:2019-12-04 标题:Methods and compositions for synthesis of therapeutic nanoparticles 发明人:WYENT EMILY A; BLUMENFELD CARL M; LAMM ROBERT J 权利人:DANTARI INC 摘要:Improved methods and reactants for the chemical synthesis of therapeutic nanoparticles are provided. The nanoparticles comprise a polymeric core, to which is attached one or more homing molecules and one or more therapeutic agents. Improvements in speed, yield and purity are attained using the methods disclosed herein.
专利号:US-6867306-B2 优先权日:2001-01-19 标题:Process for the synthesis of atorvastatin form v and phenylboronates as intermediate compounds 发明人:SRINATH SUMITRA; MATHEW JOY; UJIRE SANDHYA; SRIDHARAN MADHAVAN; SAMBASIVAM GANESH 权利人:BIOCON LTD 摘要:The present invention discusses a novel process for the synthesis of [R-(R*,R*)]-2-(4-fluorophenyl)-B,D-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium, atorvastatin. The compound so prepared is useful as inhibitor of the HMG-CoA reductase and may thus be used as hypolipidemic and hypocholesterolemic agent.
专利号:US-2023212216-A1 优先权日:2019-12-20 标 题:Synthesis of lactone derivatives and their use in the modification of proteins 发明人:MORRIS ALEXANDER REDFERN; SUTOV GRIGORIJ; BRUNE KARL DIETRICH 权利人:GENIE BIOTECH UK LTD 摘要:Site-specific modifications of proteins are desirable in biotechnological applications such as biopharmaceuticals, immunotherapy, vaccines, and are useful in chemical biology. Gluconoylation is a non-enzymatic, covalent, post-translational modification commonly observed on N-terminal His-Tags bearing proteins. We synthesized glucono-1,5-lactone derivatives, including azido variants for selective acylation. High yield acylation is achieved by simply mixing derivatives with target protein amidst diverse conditions of temperatures, aqueous buffers, excipients, or complex cell lysate.
专利号:WO-2011106986-A1 优先权日:2010-03-02 标题:Inhibitors of hepatitis c virus ns5b polymerase 发明人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO 权利人:MERCK SHARP & DOHME; MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO 摘要:Compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and /or viral production in a cell-based system. Wherein Z, R 30 , R 40 , R 50 and R 60 of compounds of formula (I) are herein defined as in the description.
专利号:US-7902196-B2 优先权日:2005-03-17 标 题 :Synthesis of avrainvillamide, strephacidin B, and analogues thereof 发明人:MYERS ANDREW G; HERZON SETH B; WULFF JEREMY EARLE; SIEGRIST ROMAIN; SVENDA JAKUB; ZAJAC MATTHEW ALLEN 权利人:HARVARD COLLEGE 摘要:The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The α,β-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores. The compounds of the invention may be used in the treatment of diseases such as cancer, autoimmune diseases, and bacterial infection.
[参考文献]: Azza H Rageh, Et Al. Boronate Affinity-Assisted Mekc Separation Of Highly Hydrophilic Urinary Nucleosides Using Imidazolium-Based Ionic Liquid Type Surfactant As Pseudostationary Phase. Electrophoresis. 2015 Mar;36(5):784-95. [参考文献]: Chiaki Miyamoto, Et Al. Kinetic Evidence For High Reactivity Of 3-Nitrophenylboronic Acid Compared To Its Conjugate Boronate Ion In Reactions With Ethylene And Propylene Glycols. Inorg Chem. 2008 Mar 3;47(5):1417-9. [参考文献]: Chun-Ping Lu, Et Al. Nitrophenylboronic Acids As Highly Chemoselective Probes To Detect Hydrogen Peroxide In Foods And Agricultural Products. J Agric Food Chem. 2011 Nov 9;59(21):11403-6. [参考文献]: Claire Kaiser, Et Al. Electrokinetic Probes For Single-Step Screening Of Polyol Stereoisomers: The Virtues Of Ternary Boronate Ester Complex Formation. Chem Commun (Camb). 2008 Jan 21:(3):338-40. [参考文献]: Fan Fei, Et Al. Direct Analysis Of Polyols Using 3-Nitrophenylboronic Acid In Capillary Electrophoresis: Thermodynamic And Electrokinetic Principles Of Molecular Recognition. Anal Bioanal Chem. 2010 Oct;398(3):1349-56.
合成参考文献
摘要:Black, D. A.; Fagnou, K., Science of Synthesis, (2010) 45, 555. 摘要:Sartori, G.; Maggi, R., Science of Synthesis, (2010) 47, 520. 摘要:Hall, D. G.; Zheng, H., Science of Synthesis Knowledge Updates, (2011) 4, 84. 摘要:Hall, D. G.; Zheng, H., Science of Synthesis Knowledge Updates, (2011) 4, 97. 摘要:Hall, D. G.; Zheng, H., Science of Synthesis Knowledge Updates, (2011) 4, 92.