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:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
专利号:US-2009131498-A1 优先权日:2005-01-18 标题 :Enantioselective Synthesis of Merrilactone and Its Analogs 发明人:DANISHEFSKY SAMUEL J; MENG ZHAOYANG; BIRMAN VLADIMIR 权利人:DANISHEFSKY SAMUEL J; MENG ZHAOYANG; BIRMAN VLADIMIR 摘要:This invention provides a method of synthesizing enantioenriched merrilactone A and enantiopure merrilactone A, as well as an improved method of synthesizing racemic merrilactone. This invention also provides intermediate compounds and methods of treating peripheral neuropathies
专利号:US-4298752-A 优先权日:1980-09-19 标题:Cycloadduct precursors of cantharidin and method 发明人:DAUBEN WILLIAM G; KESSEL CARL R; TAKEMURA KAZUO H 权利人:UNIV CALIFORNIA 摘要:Novel cycloadducts are provided which may be formed between furan and 2,5-dihydrothiophene-3,4-dicarboxylic anhydride at elevated pressure. One of these cycloadducts is useful in a synthesis of cantharidin. Another yields a novel isomeric cantharidin.
专利号:WO-2025124564-A1 优先权日:2023-12-15 标题:Polyester synthesis based on aspartic acid modification 发明人:ZHANG KECHUN; CHEN XI; LEI TENGFEI; LIU SHENGYANG 权利人:MINT BIOTECHNOLOGIES CO LTD 摘要:Provided in the present invention is polyester synthesis based on aspartic acid modification. A monomer of a unique structure of an imide ring is obtained based on aspartic acid and a dibasic acid likely to be cyclized, the monomer is based on the aspartic acid, can be derived from biomass, is low in cost and renewable, meets the requirement of sustainable development, and the unique structure of the monomer can regulate and control various properties of polyester materials, such as the mechanics, temperature resistance, hydrophilicity and hydrophobicity, and crystallization.
参考标题:Synthesis Of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, And 2-Pyrazolylbenzohydrazide Via 3-Substituted 3-Hydroxyisoindolin-1-Ones 作者:Hanh Nho Nguyen,Victor J. Cee,Holly L. Deak,Bingfan Du,Kathleen Panter Faber,Hakan Gunaydin,Brian L. Hodous,Steven L. Hollis,Paul H. Krolikowski,Philip R. Olivieri,Vinod F. Patel,Karina Romero,Laurie B. Schenkel,Stephanie D. Geuns-Meyer |发布日期:2012.4.20 摘要:Hydrazine, Followed By Chlorination With Pocl3. We Have Also Discovered Two Novel Transformations Of 3-Vinyl- And 3-Alkynyl-3-Hydroxyisoindolinones. Addition Of Vinyl Organometallic Reagents To N,N-Dimethylaminophthalimide (8A) Provided Dihydrobenzoazepinediones 15A-15C Via The Proposed Ring Expansion Of 3-Vinyl-3-Hydroxyisoindolinone Intermediates. 3-Alkynyl-3-Hydroxyisoindolinones React With Hydrazine And
合成参考文献
参考文献:10.1038/ja.2011.55 摘要:Chen X, Zhu X, Ding Y, Shen Y. Antifungal activity of tautomycin and related compounds against Sclerotinia sclerotiorum. J Antibiot (Tokyo). 2011 Aug;64(8):563–9. doi: 10.1038/ja.2011.55.