专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:WO-9707129-A1 优先权日:1995-08-18 标题 :Solution synthesis of peripheral acting analgesic opioid tetrapeptides 发明人:RINALDI NICHOLAS 权利人:IAF BIOCHEM INT; RINALDI NICHOLAS 摘要:This invention provides a bulk scale process for the solution synthesis of enantiomerically pure peripherally acting analgesic opioid tetrapeptides corresponding to formula (I): Tyr-(D)R1-R2-R3-NH2, where R1 is Ala or Arg; R2 is Phe or Phe(p-F); and R3 is Phe or Phe(p-F). A new and unique multi-step process is disclosed comprising the joining of two dipeptides using standard solution phase synthesis techniques, but adjusting the individual factors (e.g., solvents, activating agents, neutralizing agents etc.), to minimize racemization of the second amino acid. Tremendous cost efficiencies are achieved due to elimination of traditional sequential blocking-deblocking cycles and multiple chromatographic purification steps, which also enables these simple kilogram quantity methods to be scaled up to commercial production.
专利号:US-8101804-B2 优先权日:2006-07-28 标 题 :Process for the synthesis of (E)-stilbene derivatives which makes it possible to obtain resveratrol and piceatannol 发明人:SCHOUTEETEN ALAIN; JUS SEBASTIEN; VALLEJOS JEAN-CLAUDE 权利人:SCHOUTEETEN ALAIN; JUS SEBASTIEN; VALLEJOS JEAN-CLAUDE; CLARIANT SPECIALTY FINE CHEM F 摘要:A subject-matter of the present invention is a novel process for the synthesis of (E)-stilbene derivatives targeted at obtaining in particular resveratrol and piceatannol.
专利号:US-6121054-A 优先权日:1997-11-19 标 题 :Method for separation of liquid and solid phases for solid phase organic syntheses 发明人:LEBL MICHAL 权利人:TREGA BIOSCIENCES INC 摘要:A simple, efficient apparatus and method for separation of solid and liquid phases useful in methods of high-throughput combinatorial organic synthesis of large libraries or megaarrays of organic compounds is disclosed. The apparatus and method are useful, whether as part of an automated, robotic or manual system for combinatorial organic synthesis. In a preferred embodiment, an apparatus and method of removal of liquid phase from solid phase compatible with microtiter plate type array(s) of reaction vessels is disclosed.
专利号:US-9581601-B2 优先权日:2011-05-18 标题:Method of detection of amino acid sequence and/or identification of peptides and proteins, by use of a new derivatization reagent and synthesis of 5-formyl-benzene-1,3-disulphonic acid as derivatization reagent 发明人:CINDRIC MARIO; HAMERSAK ZDENKO; DODIG IVANA 权利人:CINDRIC MARIO; HAMERSAK ZDENKO; DODIG IVANA; RUDJER BOSKOVIC INST 摘要:Present invention refers to a novel and improved method of derivatization and detection of amino acid sequence and/or identification of proteins, peptides by a new derivatization compound. Precisely, the method discloses a novel approach to derivatization of peptides or proteins by compounds comprising two or more sulfonyl groups and analysis of derivatized analytes in negative mode of operation of mass spectrometer. This method allows unambiguous analysis of amino acid sequence of long-chain peptides/proteins. Also, the invention discloses a novel synthesis procedure of 5-formyl-benzene-1,3-disulphonic acid as derivatization compound.
专利号:US-7705188-B2 优先权日:2002-04-10 标 题:Structural modification of resveratrol: sodium resverastatin phosphate 发明人:PETTIT GEORGE R; GREALISH MATTHEW P 权利人:UNIV ARIZONA 摘要:Described herein are novel compounds having antineoplastic and antimicrobial activity, obtained via structural modifications of resveratrol and combretastatin A-4, methods for synthesis of these compounds, and their use in pharmaceutical composition and for use in the treatment of mammals having cancer. Examples of the novel compounds are: (Z)- and (E)-3,4′,5-trimethoxystilbene (4a, 4b); (Z)- and (E)-3,5-dimethoxy-4′-hydroxystilbene (14c, 14d); (Z)- and (E)-3-hydroxy-4′,5-dimethoxystilbene (14g, 14h); (Z)- and (E)-3,5-dihydroxy-4′-methoxy-stilbene (14k, 14l); sodium resverastatin dibenzyl phosphate ((Z)-3,5-dimethoxy-4-[O-bis(benzyl)phosphoryl]-stilbene) (14m); and sodium resverastatin phosphate (14n).
参考标题:Efficient Syntheses Of Korupensamines A, B And Michellamine B By Asymmetric Suzuki-Miyaura Coupling Reactions 作者:Guangqing Xu,Wenzhen Fu,Guodu Liu,Chris H. Senanayake,Wenjun Tang |发布日期:2014.1.15 摘要:Efficient Asymmetric Suzuki-Miyaura Coupling Reactions Are Employed For The First Time In Total Syntheses Of Chiral Biaryl Natural Products Korupensamine A And B In Combination With An Effective Diastereoselective Hydrogenation, Allowing Ultimately A Concise And Stereoselective Synthesis Of Michellamine B. Chiral Monophosphorus Ligands L1-3 Are Effective For The Syntheses Of A Series Of Functionalized
合成参考文献
参考文献:10.1002/rcm.4427 摘要:Camont L, Collin F, Marchetti C, Jore D, Gardes-Albert M, Bonnefont-Rousselot D. Liquid chromatographic/electrospray ionization mass spectrometric identification of the oxidation end-products of trans-resveratrol in aqueous solutions. Rapid Commun Mass Spectrom. 2010 Mar 15;24(5):634–42. doi: 10.1002/rcm.4427.