2-(10-羟基癸基)-5,6-二甲氧基-3-甲基苯酚置于potassium Nitrososulfonate体系中,用 Sodium Hydroxide 作为反应溶剂,化学反应 1.0H,以67%的收率获得产物艾地苯醌 参考文献:Synthesis Of Quinones Having Carboxy-And Hydroxy-Alkyl Side Chains,And Their Effects On Rat-Liver Lysosomal Membrane. 标题:Synthesis Of Quinones Having Carboxy-And Hydroxy-Alkyl Side Chains,And Their Effects On Rat-Liver Lysosomal Membrane. 摘要:为了研究辅酶q,α-生育酚和叶绿醌(ia,B,C,Iia,B,C)的代谢产物结构活性关系,将3-羧基-2-丁烯基(iiia,B,C),6-羟基-3-甲基-2-己烯基(iva,B,C),4-羟基-3-甲基丁基(va,B),4-羟基-3-甲基-2-丁烯基(vib,C),ω-羧基烷基(viia,B,C)和ω-羟基烷基(viiia,B)侧链引入到2,3-二甲氧基-5-甲基-1,4-苯醌和2,3,5-三甲基-1,4-苯醌的6-位以及2-甲基-1,4-萘醌的3-位.研究了这些醌类化合物对大鼠肝脏溶酶体膜稳定性和牛心磷酸二酯酶活性的影响.苯醌衍生物(viia,B)的这些活性之间观测到了非常好的相关性. DOI:10.1248/cpb.30.2797
专利号:US-2024336586-A1 优先权日:2021-07-29 标题:Methods for synthesis of racemic, scalemic, and chiral alpha-tocotrienol quinone 发明人:GIANNOUSIS PETER; MOLLARD PAUL; GOUDEDRANCHE SEBASTIEN; KARASAWA TOMOYA 权利人:PTC THERAPEUTICS INC 摘要:The application discloses methods useful for the synthesis of racemic, scalemic, and chiral alpha-tocotrienol quinone, including synthetic intermediates and methods for making said synthetic intermediates.
专利号:WO-2018171278-A1 优先权日:2017-03-24 标 题:Use of compound ss-31 in preparation of drugs for treating friedreich's ataxia and related diseases 发明人:LI KUANYU 权利人:NANJING UNIVERSITY OF TECHNOLOGY 摘要:Disclosed is the use of compound Szeto-Schiller-31 (SS-31) in the preparation of drugs for treating Friedreich's ataxia (FRDA) and related diseases. The present invention belongs to the pharmaceutical field, and particularly relates to the use of SS-31 in the treatment of the FRDA disease. The inventor of the present invention has found, through experiments, that SS-31 up-regulates the expression of the frataxin (FXN) in cells of FRDA patients at the translational level; regulates the iron metabolism in cells of FRDA patients; promotes the synthesis of iron-sulfur clusters in mitochondria; improves the mitochondrial function; reduces the production of ROS in patient's cells; and enhances the ability of cells to resist oxidative stress. The results show that SS-31 has a potential value in the treatment of FRDA.
专利号:US-8293290-B2 优先权日:2003-04-08 标题:Annatto extract compositions, including geranyl geraniols and methods of use 发明人:TAN BARRIE 权利人:TAN BARRIE; AMERICAN RIVER NUTRITION INC 摘要:Annatto extract composition (AEC), including cis and trans geranyl geraniols (GG) and tocopherol-free C-5 unsubstituted tocotrienols (T3), increases the de novo synthesis of intermediate isoprenoid and distal protein products, including endogenous coenzyme Q10 (CoQ10), dolichols (DL) and all subsequent GG-prenylated and DL-glycosylated proteins, including GG-porphyrinated hemes. This intermediate and distal product replenishment by AEC reverses maladies of myotoxicity (of both drug and non-drug origins), including maladies that affect the muscle, kidney, eye, GI tract and skin, nerve, blood, and CoQ10-related syndromes of energetics and LDL protection. AEC anabolically increases the endogenous de novo CoQ10 synthesis via GG elongation/prenylation of side-chain and conversely CoQ10 catabolically increases the endogenous de novo GG synthesis via beta-oxidation of CoQ10. Also, such AEC decreases de novo synthesis and increases disposal of triglycerides (TG) in humans via PPAR activation and SREBP deactivation. Such drop in TG by AEC reverses maladies of insulin resistance (IR) and metabolic syndrome (MS), prediabetes, diabetes and diabetes-related cardiovascular diseases (CVD). GG activates PPAR and down regulates SREBP transcription factors. This AEC, containing GG, inhibits cancer growth whether or not GG involvement in protein prenylation is required.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-10799441-B2 优先权日:2011-06-06 标题:Skin treatments containing pyrroloquinoline quinone (PQQ) esters and methods of preparation and use thereof 发明人:LEWIS II JOSEPH ABERNATHY; DINARDO JOSEPH C 权利人:LEWIS II JOSEPH ABERNATHY; DINARDO JOSEPH C; PCR TECH HOLDINGS LC 摘要:The present invention relates to cosmetic or dermatological compositions containing PQQ or its esters, methods of treating or promoting skin changes by topical application of these compositions, and methods of synthesis of PQQ esters. The PQQ ester-containing compositions of the present invention are unexpectedly effective in treating skin, particularly with respect to skin tolerance. When included in a topical composition, the PQQ esters of the present invention have an antioxidant effect that is useful in treating a skin change.
专利号:US-2011263720-A1 优先权日:2010-03-09 标 题 :Synthesis of alpha-tocopherolquinone derivatives, and methods of using the same 发明人:PAISLEY STEVEN D; LEPREE JASON M; HAWI AMALE; ECKHOFF MICHAEL 权利人:PENWEST PHARMACEUTICALS CO 摘要:The present invention is directed to a method of synthesizing a compound of Formula I: n n n n n n n n n n the method comprising oxidizing alpha-tocopherol with a metal salt oxidizing agent to form the compound of Formula I, wherein the stoichiometric ratio (mol/mol) of metal salt oxidizing agent/alpha-tocopherol is 1.6 to 4. The invention is also directed to a method of synthesizing a compound of Formula I, the method comprising (a) hydrolyzing alpha-tocopheryl acetate in the presence of a base; (b) neutralizing the hydrolyzing of (a), thereby forming alpha-tocopherol; and (c) oxidizing the alpha-tocopherol of (b) with a metal salt oxidizing agent to form the compound of Formula I, wherein the stoichiometric ratio (mol/mol) of metal salt oxidizing agent/alpha-tocopherol is 1.6 to 4.
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合成参考文献
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