乙醛置于氨体系中,用 水 作为反应溶剂,化学反应生成 2-氨基乙醛 参考文献:Solvent Effects On Equilibria Of Addition Of Nucleophiles To Acetaldehyde And The Hydrophilic Character Of Diols 标题:Solvent Effects On Equilibria Of Addition Of Nucleophiles To Acetaldehyde And The Hydrophilic Character Of Diols 摘要: DOI:10.1021/ja00343A044
专利信息
专利号:US-2004242897-A1 优先权日:2002-07-31 标题 :Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:WO-2004011474-A1 优先权日:2002-07-31 标题:Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K 权利人:ISIS PHARMACEUTICALS INC; GUZAEV ANDREI P; MANOHARAN MUTHIAH; RAVIKUMAR VASULINGA T; KUMAR RAJU K 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotide and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-6653468-B1 优先权日:2002-07-31 标 题 :Universal support media for synthesis of oligomeric compounds 发明人:GUZAEV ANDREI P; MANOHARAN MUTHIAH 权利人:ISIS PHARMACEUTICALS INC 摘要:Compounds for the synthesis of oligomeric compounds, particularly oligonucleotides and oligonucleotide mimetics, are provided. In addition, methods for functionalizing a support medium with a first monomeric subunit and methods for the synthesis of oligomeric compounds utilizing the novel compounds bound to support media are provided.
专利号:US-10364262-B2 优先权日:2012-07-17 标 题 :Method for the synthesis of N-phosphonomethyliminodiacetic acid 发明人:DEVAUX ALBERT; BURCK SEBASTIAN; NOTTE PATRICK 权利人:MONSANTO TECHNOLOGY LLC 摘要:A method for synthesis of N-phosphonoalkyliminodiacetic acid or derivatives thereof by forming a reaction mixture having an acid catalyst, a compound of the following general formula R1—CH2—NX—CH2—R2 and a compound having one or more P—O—P anhydride moieties to form a compound having a formula R1—CH2—N(—CH2PO3R32)(—CH2—R2) wherein in R1—CH2—NX—CH2—R2: X is —CH2—OH or —CH2—COOH; R1 and R2 are independently selected from the group consisting of nitrile, C1-C4 alkyl carboxylate, and carboxylic acid for when X is —CH2—OH, or R1 and R2 are both carbonyl groups linked by a hydrogen substituted nitrogen atom or a C1-C4-alkyl substituted nitrogen atom; and R3 is H, an alkyl group, or an aryl group; the anhydride moieties in the P—O—P anhydride compound have one P atom at the oxidation state (+III) and one P atom at the oxidation state (+III) or (+V); and 2) hydrolyzing the mixture to form N-phosphonomethyliminodiacetic acid or one of its derivatives.
专利号:US-7888337-B2 优先权日:2007-08-31 标 题 :Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity 发明人:WONG CHI-HUEY; FANG JIM-MIN; SHIE JIUN-JIE; CHENG YIH-SHYUN EDMOND; JAN JIA-TSRONG 权利人:ACADEMIA SINICA 摘要:Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5 -cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.
专利号:US-9676799-B2 优先权日:2012-07-17 标 题 :Method for the synthesis of N-(phosphonomethyl)glycine 发明人:BURCK SEBASTIAN; BRUYNEEL FREDERIC; NOTTE PATRICK 权利人:STRAITMARK HOLDING AG 摘要:A method for the synthesis of N-(phosphonomethyl)glycine or one of its derivatives selected from the group consisting of its salts, its phosphonate esters, or its phosphonate ester salts, which includes the steps of: a) forming, in the presence an acid catalyst, a reaction mixture having 2,5-diketopiperazine, formaldehyde and a compound including one or more P-0-P anhydride moieties, the moieties having one P atom at the oxidation state (+III) and the other P atom at the oxidation state (+III) or (+V), to form N,N′-bisphosphonomethyl-2,5-diketopiperazine, its mono- to tetra phosphonate esters, the dehydrated forms of N,N′-bisphosphonomethyl-2,5-diketopiperazine and the phosphonate esters of its dehydrated forms; and b) hydrolyzing the N,N′-bisphosphonomethyl-2,5-diketopiperazine, its dehydrated forms or their phosphonate esters to obtain N-(phosphonomethyl)glycine or one of its derivatives selected from the group consisting of its salts, its phosphonate esters and its phosphonate ester salts.
参考标题:Synthesis Of Naphthazarin Derivatives And Identification Of Novel Thioredoxin Reductase Inhibitor As Potential Anticancer Agent 作者:Junmin Zhang,Yaping Liu,Danfeng Shi,Guodong Hu,Baoxin Zhang,Xinming Li,Ruijuan Liu,Xiao Han,Xiaojun Yao,Jianguo Fang |发布日期:2017.11 摘要:Drug Targets. We Report Here The Synthesis Of A Panel Of Naphthazarin Derivatives And Discovery Of 2-Methyl-5,8-Dihydroxy-1,4-Naphthoquinone (3, 2-Methylnaphthazarin) As A Potent Cytotoxic Agent With A Submicromolar Half Maximal Inhibitory Concentration To The Human Promyelocytic Leukemia Hl-60 Cells. Mechanism Studies Reveal That The Compound Selectively Inhibits Trxr To Induce Oxidative Stress-Mediated
合成参考文献
参考文献:10.3390/md9061157 摘要:Aiello A, Fattorusso E, Imperatore C, Irace C, Luciano P, Menna M, Santamaria R, Vitalone R. Zorrimidazolone, a bioactive alkaloid from the non-indigenous mediterranean stolidobranch Polyandrocarpa zorritensis. Mar Drugs. 2011;9(6):1157–65. 参考文献:10.1107/s160053681100852x 摘要:Li J. 2-Hy-droxy-ethanaminium 3,4,5,6-tetra-bromo-2-(meth-oxy-carbon-yl)benzoate methanol monosolvate. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o866.