3-氟邻苯二甲酸置于乙酸酐体系中,化学反应 5.0H,以92%的收率获得产物3-氟邻苯二甲酸酐 参考文献:Design,Synthesis,And Biological Evaluation Of Proteolysis Targeting Chimeras (Protacs) For The Dual Degradation Of Igf-1R And Src 标题:Design,Synthesis,And Biological Evaluation Of Proteolysis Targeting Chimeras (Protacs) For The Dual Degradation Of Igf-1R And Src 摘要:开发了一个专注于降解与各种癌症相关的igf-1R和src蛋白的protac文库.通过将不同的抑制剂战斗单元和e3连接酶(crbn)招募-泼美度胺与不同的连接剂相结合,合成了具有igf-1R和src降解潜力的protac.设计的protacs 12A-B在各种细胞实验中以低微摩尔效力(1-5μm)抑制了mcf7和a549癌细胞的增殖和迁移. DOI:10.3390/molecules25081948
专利号:US-4255594-A 优先权日:1979-09-18 标题 :Hydrogenation of halogen-containing carboxylic anhydrides 发明人:NOVOTNY MIROSLAV 权利人:ALLIED CHEM 摘要:A process is described for the heterogeneous hydrogenation of haloalkyl, halocycloalkyl or haloaryl carboxylic anhydrides to the corresponding primary alcohols. In the haloalkyl or halocycloalkyl carboxylic anhydrides at least one halogen is in the alpha-position relative to the carboxylic anhydride grouping. The hydrogenation can be carried out in the liquid or vapor phase in the presence of a supported or unsupported catalyst comprising a member of the group consisting of rhodium, iridium, metal oxides thereof, or mixtures thereof. In the liquid phase, the hydrogenation can be carried out batchwise under mild conditions of temperature and pressure, preferably at about 50°-150° C. and about 5-15 atmospheres, in an atmosphere containing hydrogen gas. A preferred embodiment is the hydrogenation of trifluoroacetic anhydride in the liquid phase to 2,2,2-trifluoroethanol, said alcohol being useful as an intermediate in the synthesis of the anesthetic, isoflurane, CF 3 CHClOCHF 2 .
专利号:US-2010323953-A1 优先权日:2007-01-08 标 题:Macrocyclic hepatitis c protease inhibitors 发明人:CAMPBELL DAVID ALAN; HEPPERLE MICHAEL E; WINN DAVID T; BETANCORT JUAN MANUEL 权利人:PHENOMIX CORP 摘要:The present invention provides novel macrocyclic compounds that mimic peptide substrates of the hepatitis C viral protease and inhibit the viral protease, more particularly as inhibitors of the NS3 serine protease from hepatitis C virus. Methods for synthesis of the compounds are also provided. The compounds find utility as antiviral agents directed at hepatitis C. The invention further provides methods of employing such inhibitors, alone or in combination with other therapeutic agents, to treat hepatitis C infection in a subject in need of such treatment.
专利号:US-7268237-B2 优先权日:2005-03-11 标题:Direct dianhydride synthesis 发明人:BRUNELLE DANIEL JOSEPH; CELLA JAMES ANTHONY; YE QING; CHAN KWOK PONG 权利人:GEN ELECTRIC 摘要:This invention is related to a method for making diether dianhydrides by the reaction of halophthalic anhydride and a metal salt of an aromatic dihydroxy compound in the presence of a solvent and a phase transfer catalyst. Typical phase transfer catalyst include guanidium salts, aminopyridinium salts, or phosphazenium salts.
专利号:WO-2024035626-A1 优先权日:2022-08-11 标 题:Halophthalimide compounds and methods of use against tbi, inflammatory disorder, autoimmune disorder, neurodegenerative disease or viral infection 发明人:GREIG NIGEL; LUO WEIMING; TWEEDIE DAVID; SCERBA MICHAEL; LECCA DANIELA; HSUEH SHIH CHANG; KIM DONG SEOK 权利人:US HEALTH; AEVISBIO INC 摘要:Halophthalimides are disclosed. The halophthalimides may inhibit TNF-α activity, TNF-α synthesis, inflammation, inducible nitric oxide synthase, SARS-CoV-2 virus, or any combination thereof. The halophthalimides may be administered to a subject with a traumatic brain injury, an inflammatory disorder, an autoimmune disorder, a neurodegenerative disease, a viral infection, or any combination thereof. The disclosed halophthalimides have a structure according to Formula (I), or a stereoisomer or pharmaceutically acceptable salt, solvate, or hydrate thereof,
专利号:WO-03033594-A1 优先权日:2001-10-10 标题 :Thermoplastic moulding materials based on polyarylene ether sulfones and polyamides 发明人:WEBER MARTIN; CHAROENSIRISOMBOON PIYADA 权利人:BASF AG; WEBER MARTIN; CHAROENSIRISOMBOON PIYADA 摘要:The invention relates to moulding materials containing A) between 1 and 98.5 wt. % of at least one polyarylene ether sulfone, B) between 1 and 98.5 wt. % of at least one thermoplastic polyamide, C) between 0.5 and 30 wt. % of at least one polyarylene ether sulfone containing between 0.01 and 10 wt. % - in relation to the total weight of constituent C - of units which are derived from a compound X comprising at least three hydroxy or halogen substituents which are independently directly linked to an aromatic ring and can be substituted under the conditions of a polyarylene ether sulfone synthesis, in addition to anhydride groups, D) between 0 and 60 wt. % of at least one filler, E) between 0 and 40 wt. % of at least one impact-resistant modified rubber, and F) between 0 and 40 wt. % of at least one different additional additive, the weight per cent of constituents A to F amounting to 100 %. The invention also relates to methods for producing said moulding materials, to the uses of the same, and to moulded parts, films or fibres which can be obtained from said moulding materials.
专利号:RU-2200159-C2 优先权日:1998-03-16 标 题 :Derivatives of 2-(2,6-dioxopiperidine-3-yl)isoindoline, their synthesis and application as inhibitors of inflammatory cytokines
[参考文献]: M H Norman, Et Al. Structure-Activity Relationships Of A Series Of Substituted Benzamides: Potent D2/5-Ht2 Antagonists And 5-Ht1A Agonists As Neuroleptic Agents. J Med Chem. 1996 Mar 1;39(5):1172-88.
合成参考文献
摘要:Maier, M. E., Science of Synthesis, (2007) 20, 1528.