N-(3-羟丙基)氨基甲酸叔丁酯置于重铬酸吡啶体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 Boc-Beta-丙氨酸 参考文献:New Anti-Hiv Derivatives: Synthesis And Antiviral Evaluation 标题:New Anti-Hiv Derivatives: Synthesis And Antiviral Evaluation 摘要:A Small Focused Library Of 18 Compounds Incorporating The Motif 1,3-(N,N'-Dibenzyl)Diamino-2-Propanol Has Been Synthesized,Using Adapted Synthetic Methodologies. These Series Of Compounds Were Evaluated For Their In Vitro Anti-Hiv Activity On Infected Mt(4) Cells (Syncytium Formation Observation). Some Of The New Synthesized Compounds Show Potent Anti-Hiv Activities. Ec(50) Values For Compounds (31,40,34,37 And 46) Range From 0.1 To 1 Mu M. In Order To Determine At Which Level These New Derivatives Interfere With The Hiv Replicative Cycle,Inhibition Assays On Recombinant Hiv Protease And Hiv Integrase Have Been Performed. None Of The Compounds Were Found Active On These Two Enzymatic Targets. Experiments Are In Progress In Order To Identify Their Biological Target Within The Hiv Replicative Cycle. (C) 2000 Elsevier Science Ltd. All Rights Reserved. DOI:10.1016/s0968-0896(00)00055-9
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-2024400608-A1 优先权日:2021-09-03 标题:Synthesis of bicycle toxin conjugates, and intermediates thereof 发明人:WITTY DAVID; LIMB DARREN; MIN BYOUNG JOON; HE LIWEN; SANDERS WILLIAM J; NNANABU ERNEST OBINNA 权利人:BRICYCLETX LTD 摘要:The present invention relates to Bicycle toxin conjugates, methods for preparation, and methods of use for treating cancer.
专利号:US-2009099061-A1 优先权日:2006-01-27 标 题:Synthesis of carotenoid analogs or derivatives with improved antioxidant characteristics 发明人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 权利人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 摘要:A method is described for synthesizing and administering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.
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-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-5783577-A 优先权日:1995-09-15 标题 :Synthesis of quinazolinone libraries and derivatives thereof 发明人:HOUGHTEN RICHARD A; OSTRESH JOHN M 权利人:TREGA BIOSCIENCES INC 摘要:The present invention provides synthetic combinatorial libraries of organic compounds based on the quinazolinone ring.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1095.
合成参考文献
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