专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
专利号:US-7169589-B2 优先权日:2000-07-28 标题 :Silicatein-mediated synthesis of amorphous silicates and siloxanes and use thereof 发明人:MUELLER WERNER E G; SCHROEDER HEINZ C; LORENZ BERND; KRASKO ANATOLI 权利人:MUELLER WERNER E G; SCHROEDER HEINZ C; LORENZ BERND; KRASKO ANATOLI 摘要:Silicatein is an enzyme of silicate-forming organisms used for the synthesis of their silicate scaffold. The present invention relates to the use of highly-expressed and highly active recombinant silicatein, silicatein isolated from natural sources after gene induction as well as silicatein-fusion proteins for the synthesis of amorphous silicon dioxide (silicic acids and silicates), siloxanes as well as modification of these compounds and their technical use.
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:US-5668285-A 优先权日:1986-10-31 标 题 :Total synthesis of northebaine, normophine, noroxymorphone enantiomers and derivatives via N-Nor intermediates 发明人:RICE KENNER CRALLE; NEWMAN AMY HAUCK 权利人:US HEALTH 摘要:The invention involves a method of making key intermediates useful in the synthesis of many opiate narcotics and antagonists and agonists; and the non-opiate enantiomers thereof which have potent antitussive properties. The synthesis starts from either the natural or unnatural enantiomer of nordihydrocodeinone and produces 8, 14-dihydronorthebaine, the diketal of 7-bromonordihydrocodeinone, northebaine, norcodeinone diketal and 14-hydroxynorcodeinone intermediates without the necessity of leaving the N-nor structure. The syntheses have fewer steps than previous methods, and also have high yields.
专利号:US-5571677-A 优先权日:1993-07-02 标题:Convergent synthesis of branched and multiply connected macromomolecular structures 发明人:GRYAZNOV SERGEI M 权利人:LYNX THERAPEUTICS INC 摘要:The invention provides methods and compositons for convergent synthesis of branched polymers useful as molecular probes. The invention also includes several novel branched polymeric structures particularly useful for detecting target polynucleotides. Branched polymers of the invention comprise at least two branches: at least one branch is a target binding moiety capable of specifically binding to a target molecule of interest and one or more branches are signal generation moities capable of directly or indirectly generating a detectable signal. In accordance with the method of the invention branched polymers are assembled from components having phosphorothioate groups and/or haloacyl- or haloalkylamino groups. The phosphorothioate and haloacyl- or haloalkylamino groups react rapidly and efficiently when brought into contact to form thiophosphorylacyl- or thiophosphorylalkylamino bridges which.complete the assembly of a branched polymer. The method of the invention permits thorough purification and isolation of the components prior to final assembly. Incomplete branched polymers are readily separated from the desired product by standard means. The method of the invention permits the synthesis of several novel branched polymer configurations.
专利号:WO-9532946-A1 优先权日:1994-05-27 标题 :Methods for the synthesis of 9-cis retinoids and their novel intermediates 发明人:BENNANI YOUSSEF L 权利人:LIGAND PHARM INC 摘要:Methods for the synthesis of 9-cis retinoids, novel intermediates and methods for the synthesis of cyclohexadienyne nitriles and 9-cis alkyl cisoid nitriles, as well as 9-cis retinoids made using such methods are provided.
参考文献:10.4061/2011/896567 摘要:Nakashima I, Kawamoto Y, Takeda K, Kato M. Control of Genetically Prescribed Protein Tyrosine Kinase Activities by Environment-Linked Redox Reactions. Enzyme Research. 2011 Jun 26;2011():1–10. doi: 10.4061/2011/896567. 参考文献:10.1007/978-1-61779-252-6_5 摘要:Lafanechère L, Job D. Preparation of pure tyrosinated or detyrosinated tubulin isoforms. Methods Mol Biol. 2011;777():71–86. doi: 10.1007/978-1-61779-252-6_5.