专利号:US-9376461-B2 优先权日:2011-06-06 标 题:Non-enzymatic synthesis of O-acetyl-ADP-ribose and analogues thereof 发明人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B 权利人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B; GLAXOSMITHKLINE LLC 摘要:Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2′- and 3′-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.
专利号:US-9199913-B2 优先权日:2011-04-25 标 题:Process for continous flow synthesis of beta-amino crotonate 发明人:KULKARNI ARVIND A; JOSHI ANNA R; JOSHI RAMESH R 权利人:KULKARNI ARVIND A; JOSHI ANNA R; JOSHI RAMESH R; COUNCIL SCIENT IND RES 摘要:Beta aminocrotonates are important intermediates for the synthesis of Ca channel blockers. The processes available in the art are batch processes with yields about 85%. There are no continuous processes available for the synthesis of such compounds. This gap in the art is addressed by the invention by disclosing a continuous process resulting in high yields of beta amino crotonates.
专利号:US-4064150-A 优先权日:1976-05-26 标 题 :Synthesis of isoprenoid 1,5-dienes 发明人:KATZENELLENBOGEN JOHN A 权利人:UNIV ILLINOIS 摘要:Aliphatic acids containing an isoprenoid 1,5-diene moiety are prepared in high yields by the selective gamma alkylation of α,β-unsaturated acids with allylic electrophiles. The gamma-regioselectivity of the alkylation is controlled by the use of the dicopper(I) dienolates prepared from the α,β-unsaturated acids. The method offers a particularly facile means for synthesizing isoprenoid 1,5-diene natural products such as farnesoic acid by alkylation of senecioic acid with geranyl bromide; geranoic acid by alkylation of senecioic acid with 3,3-dimethallyl bromide; and dl-lanceol by alkylation of tiglic acid with an allylic bromide derived from dl-limonene. Such products find use in the synthesis of insect pheremones, insect juvenile hormones, and components of perfumes.
专利号:EP-1669379-B1 优先权日:2003-09-23 标 题 :3,5-dimethyl-1-adamantyl-ammonium polymeric salts and the use thereof in the form of antiviral agents 发明人:MARCHUKOV VALERY ALEKSANDROVIC; PLATONOV VITALY GEORGIEVICH; SELKOV SERGEI ALEKSEEVICH; CHERNOBROVY ALEKSANDR NIKOLAEV 权利人:AKCIJU SABIEDRIBA OLAINFARM 摘要:This invention relates to the polymeric salts of 3.5-dimethyl-1-adamantylammonium and carboxylated (co)polymers, as well as to the use of produced salts as antiviral agents. Object of the invention is the synthesis of new salts of 3.5-dimethyl-1-adamantylammonium and carboxylated (co)polymers, identification of the compounds with antiviral activity and durable action among them. The task is solved by the synthesis of salts of 3.5-dimethyl-1-adamantylammonium and water-soluble carboxylated (co)polymers of a general formula (1): nwhere m and n are mol%, m = 100 - n, nand carboxylated (co)polymers are selected from the group: nvinylaminosuccinic acid, a copolymer of vinyl alcohol and N-vinylaminosuccinic acid, a copolymer of N-vinylpyrrolidone and N-vinylaminosuccinic acid, copolymer of N-vinylpyrrolidone and crotonic acid; copolymer of N-vinylaminosuccinimide and maleic anhydride; copolymer of N-vinylpyrrolidone and maleic anhydride; polyacrylic acid A general synthesis method and synthesis examples are given for each of claimed compounds, as well as the results of identification of toxicity and comparative antiviral activity. Produced compounds are expressly identified by methods of IR analysis, elements analysis, and potentiometric titration, have quite high antiviral activity against the viruses of influenza types A and B, at that they feature durable (prolonged) action which allows using these produced salts not only as antiviral medications for sparing treatment but for prevention of viral diseases.
专利号:US-2012178961-A1 优先权日:2009-07-02 标题:Bio-derived olefin synthesis 发明人:SANDERS JOHAN PIETER MARINUS; VAN HAVEREN JACOBUS; SCOTT ELINOR; VAN ES DANIEL STEPHAN; LE NOTRE JEROME; SPEKREIJSE JURJEN 权利人:SANDERS JOHAN PIETER MARINUS; VAN HAVEREN JACOBUS; SCOTT ELINOR; VAN ES DANIEL STEPHAN; LE NOTRE JEROME; SPEKREIJSE JURJEN; UNIV WAGENINGEN; STICHTING DIENST LANDBOUWKUNDI 摘要:Disclosed is a method for the combined synthesis of at least two vinylic monomers, at least one of which being an acrylic compound, comprising subjecting a monoconjugated alkene-1-carboxylic compound to reaction with a C 2 -C 4 alkene under conditions of olefin cross-metathesis. The invention is particularly useful for extracting value from protein side streams. Upon protein hydrolysis, suitable amino acids (preferably phenylalanine or tyrosine) are subjected to reductive amination so as to form the corresponding alkene-1-carboxylic acid. Preferably after esterification and separation, this is used in cross-metathesis for the concomitant production of styrene resp. hydroxy styrene, and acrylates. The invention is applicable more widely, to the synthesis of olefins on the basis of carbohydrates, naturally occurring phenolic components, natural protein resources, or amino acids obtained from fermentations.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
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合成参考文献
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