专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-6168931-B1 优先权日:1999-03-17 标题 :Enhanced in vitro synthesis of biological macromolecules using a novel ATP regeneration system 发明人:SWARTZ JAMES R; KIM DONG-MYUNG 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Compositions and methods are provided for the enhanced in vitro synthesis of biological molecules where ATP is required for synthesis. Of particular interest is the synthesis of polymers, e.g. nucleic acids, polypeptides, and complex carbohydrates. A homeostatic system is used for production of ATP, where the required high energy phosphate bonds are generated in situ, e.g. through coupling with an oxidation reaction. The homeostatic energy source will typically lack high energy phosphate bonds itself, and will therefore utilize free phosphate in the reaction mix during generation of ATP. Since inorganic phosphate can be an inhibitory by-product of synthesis, the period of time when synthesis is maintained in vitro can be extended. The homeostatic energy source is provided in combination with an enzyme that catalyzes the creation of high energy phosphate bonds and with an enzyme that can use that high energy phosphate bond to regenerate ATP.
专利号:US-5220016-A 优先权日:1991-07-29 标 题:Synthesis of navelbine analogs 发明人:MAGNUS PHILIP D; THURSTON LEE S 权利人:UNIV TEXAS 摘要:The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-protecting group is removed to provide a 2-methoxyindole hydroxy ester which is coupled to vindoline. After removal of the amineprotecting group from the piperidinyl group, ring closure to the indole moiety provides dihydrodesethyl navelbine. Other derivatives and analogs of navelbine with potential clinical applications in cancer chemotherapy may be readily synthesized. The synthesis opens a route to a wide variety of navelbine modifications, including modifications at or near the tryptamine bridge.
专利号:US-7199257-B1 优先权日:1999-06-10 标题 :Process for the synthesis of N-(4-cyano-3-trifluoromethylphenyl)-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamide 发明人:SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; BOR ADAM; DEMETER ADAM; TRISCHLER FERENC; HORVATH JANOS; BRLIK JANOS 权利人:RICHTER GEDEON VEGYESZET 摘要:A new process is disclosed for the synthesis of racemic or optically pure N-[4-cyano-3-trifluoro-methyl-phenyl]-3[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methylpropionamide. The process includes the formation of several novel intermediates in the synthesis.
专利号:US-2006264608-A1 优先权日:2001-08-03 标题 :Bi-directional synthesis of oligoguanidine transport agents 发明人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C 权利人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C 摘要:Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.
专利号:US-7414008-B2 优先权日:2002-02-28 标 题:Catalyst for synthesis of unsaturated aldehyde, production process for said catalyst, and production process for unsaturated aldehyde using said catalyst 发明人:YUNOKI HIROMI 权利人:NIPPON SHOLONBAI CO LTD 摘要:The present invention provides: a production process for a catalyst for synthesis of an unsaturated aldehyde and/or an unsaturated carboxylic acid, which production process is suitable for producing the catalyst with good reproducibility, wherein the catalyst is excellent in activity, selectivity, and physical strength; this catalyst; and a production process for the unsaturated aldehyde and/or the unsaturated carboxylic acid by using this catalyst. The production process for the catalyst comprises the steps of: carrying out heat treatment of an aqueous solution or slurry of a starting material to thus prepare a catalyst precursor P1, wherein the starting material includes molybdenum, bismuth, and iron as essential components; thereafter adding and mixing a binder into the P1 to thus prepare a catalyst precursor P2; and molding and then calcining the P2, thereby producing the catalyst for synthesis of the unsaturated aldehyde and/or the unsaturated carboxylic acid; with the production process being characterized by involving an ignition loss ratio of the catalyst precursor P1 in the range of 10 to 40 mass % (excluding 40 mass %).
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合成参考文献
参考文献:10.1007/s12640-011-9253-z 摘要:Bavithra S, Selvakumar K, Pratheepa Kumari R, Krishnamoorthy G, Venkataraman P, Arunakaran J. Polychlorinated biphenyl (PCBs)-induced oxidative stress plays a critical role on cerebellar dopaminergic receptor expression: ameliorative role of quercetin. Neurotox Res. 2012 Feb;21(2):149–59. doi: 10.1007/s12640-011-9253-z.