专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-7094805-B2 优先权日:2001-12-14 标 题 :Total synthesis of merrilactone A 发明人:DANISHEFSKY SAMUEL J; BIRMAN VLADIMIR B 权利人:UNIV COLUMBIA 摘要:This invention provides a total synthesis of Merrillactone and Merrilactone analogues for use as neurotrophic agents in the treatment of neurodegenerative diseases. The invention also provides intermediates for use in the synthesis of Merrilactone and its analogues.
专利号:WO-2004046173-A1 优先权日:2002-11-19 标题:Scaffolds useful to the synthesis of compounds with biological activity 发明人:GIANNINI GIUSEPPE; SCOLASTICO CARLO; MANZONI LEONARDO 权利人:SIGMA TAU IND FARMACEUTI; GIANNINI GIUSEPPE; SCOLASTICO CARLO; MANZONI LEONARDO 摘要:The present invention relates to cyclic compounds having the azabicycloalkane structure. Said compounds are useful as intermediates for the synthesis of compounds with biological activity.
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.
专利号:EP-0799313-A2 优先权日:1994-12-13 标 题 :Method and reagent for treatment of arthritic conditions, induction of graft tolerance and reversal of immune responses 发明人:BEIGELMAN LEONID; STINCHCOMB DANIEL T; JARVIS THALE; DRAPER KENNETH; PAVCO PAMELA; MCSWIGGEN JAMES; GUSTOFSON JOHN; USMAN NASSIM; WINCOTT FRANCINE; MATULIC-ADAMIC JASENKA; KARPEISKY ALEXANDER; THOMPSON JAMES D; MODAK ANIL; BURGIN ALEX 权利人:RIBOZYME PHARM INC 摘要:An enzymatic nucleic acid molecule which cleaves RNA associated with development or maintenance of an arthritic condition, induction of graft tolerance or reversal of an immune response. In particular, the ribozyme sequences are directed to an mRNA encoding B7-1, B7-2, B7-3, CD40 and/or stromelysin. Also provided are ribozymes where the uracil in positions 4 and/or 7 are substituted, as well as methods for the synthesis of 2'-alkylnucleotides, 2'-O-alkylthioalkyl, or 2'-alkylthioalkylnucleotides. The application further describes a method for diprotection of RNA with aqueous ethylamine, a method for synthesis of a basic ribonucleoside mimetics, and transcription units comprising an RNA polymerase II promoter, a U6 small nuclear promoter, or an adenovirus VA1 promoter system.
专利号:US-7951905-B2 优先权日:2006-09-18 标 题 :Synthesis of carbohydrate-templated amino acids and methods of using same 发明人:SCHWEIZER FRANK; ZHANG KAIDONG; OWENS NEIL; ZHANEL GEORGE 权利人:UNIV MANITOBA 摘要:The present invention generally relates to tetrahydropyranyl-derivatized amino acids, their syntheses and their incorporation into peptides and peptidomimetics. The tetrahydropyran moiety constrains the side chain of an amino acid, thereby providing a molecule that may act as a sugar- or amino acid-mimetic as well as a scaffold for combinatorial synthesis.
参考标题:Total Synthesis And Cytotoxic Activity Of 6,8-Dimethoxy-1,3-Dimethylisoquinoline Isolated From Ancistrocladus Tectorius: A 6π-Azaelectrocyclization Approach 作者:Teodoro Kaufman,Andrea Bracca,Iván Cortés,Carla Borini Etichetti,Javier Girardini |发布日期:2019.1 摘要:Microwave-Assisted 6π-Azaelectrocyclization Completed The Sequence. Functionalized Derivatives On C-1 Were Also Prepared. The Heterocycles Exhibited Cytotoxic Activity. A Facile And Convenient Approach Toward The Total Synthesis Of 1,3-Dimethyl-6,8-Dimethoxyisoquinoline From Phloroacetophenone Is Reported. The Sequence Entailed The Selective 2,4-Di-O-Methylation And Further Triflation Of The Resulting
合成参考文献
参考文献:10.3762/bjoc.22.19 摘要:Meiners P, Melder JJ, Morack T. Arene activation via π-bond localization: concepts and opportunities. Beilstein J Org Chem. 2026;22():257–73.