专利号:US-6355826-B1 优先权日:1997-09-17 标题:Synthesis of stable nitrile oxide compounds 发明人:PARKER DANE KENTON 权利人:GOODYEAR TIRE & RUBBER 摘要:This invention discloses a process for the synthesis of stable aryl nitrile oxides which comprises the sequential steps of (1) halomethylating a halomethyl group onto a substituted aromatic compounds wherein said halomethyl group is halomethylated onto a position that is ortho to at least one of the substituent groups on the substituted aromatic compound; (2) converting the ortho halomethylated-substituted aromatic compound into an ortho-substituted aromatic aldehyde by reacting the ortho halomethylated-substituted aromatic compound with a salt selected from the group consisting of sodium 2-nitropropane and potassium 2-nitropropane in a lower alcohol solvent; (3) converting the ortho-substituted aromatic aldehyde into an ortho-substituted aromatic; and (4) converting the ortho-substituted aromatic oxime into the ortho-substituted aryl nitrile oxide by reacting the ortho-substituted aromatic oxime with an aqueous sodium hypochlorite solution.
专利号:WO-2017082924-A1 优先权日:2015-11-13 标题 :Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE TERRENCE R JR; HYMEL DAVID 权利人:THE US SECRETARY DEPT OF HEALTH & HUMAN SERVICES 摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
专利号:US-6608196-B2 优先权日:2001-05-03 标题 :Process for solid supported synthesis of pyruvate-derived compounds 发明人:WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L 权利人:GALILEO PHARMACEUTICALS INC 摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
专利号:US-7737287-B2 优先权日:2002-03-28 标 题 :Anomeric derivatives of monosaccharides 发明人:MEUTERMANS WIM; WEST MICHAEL LEO; GIANG THANH LE; ADAMSON GEORGE; SCHAFER KARL; ABBENANTE GIOVANNI 权利人:ALCHEMIA LTD 摘要:This invention relates to combinatorial libraries of potentially biologically active mainly monosaccharide compounds and to methods of preparing same. These compounds are variously functionalized, with a view to varying lipid solubility, size, function and other properties, with the particular aim of discovering a drug or drug-like compound, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of monosaccharides, variously functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of amino acid and peptide side chain units of isosteres thereof.
专利号:US-9328061-B2 优先权日:2012-03-01 标题:Simple organic molecules as catalysts for practical and efficient enantioselective synthesis of amines and alcohols 发明人:HOVEYDA AMIR H; SILVERIO DANIEL L; PILYUGINA TATIANA; TORKER SEBASTIAN; ROBBINS DANIEL 权利人:TRUSTEES BOSTON COLLEGE 摘要:The present invention provides organic molecules and methods thereof for reactions between organoboron reagents and double bonds, such as imines or carbonyls, to stereoselectively provide chiral products including amines and alcohols, entities useful for the preparation of biologically active molecules.
专利号:US-2009156828-A1 优先权日:2005-12-21 标题:Novel Compounds and Methods for Forming Taxanes and Using the Same 发明人:HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH; SUMNER CHRISTIAN; YIANNIKOUROS GEORGE PETROS; STEMPHOSKI AARON MICHAEL; WALKER DONALD G 权利人:TAPESTRY PHARMACEUTICALS INC 摘要:The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds. More particularly, the present embodiments disclosed herein relate to novel side chains, that when coupled to a taxane, are useful for the synthesis of pharmaceutically useful taxanes. Methods of forming the novel side chains and coupling them to hindered alcohols, namely taxanes resulting in useful esters are also disclosed. Various taxanes compounds are known to exhibit anti-tumor activity.
[参考文献]: Colin J Murphy, Et Al. Ullmann Coupling Mediated Assembly Of An Electrically Driven Altitudinal Molecular Rotor. Phys Chem Chem Phys. 2015 Dec 21;17(47):31931-7.
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