CAS: 30652-11-0; 3-Hydroxy-1,2-Dimethylpyridin-4(1H)-One

该化合物是一种口服活性铁色带,主要用于治疗地中海贫血和其他依赖输血的贫血病人的铁过量,其主要优势在于它能够有选择地捆绑过量的铁,形成通过尿液排出的稳定的复合体,从而减少组织中的有毒铁积聚.易腐性表现出极接近于发酵铁(Fe3+) , 并能够渗透细胞细胞内部实验室铁池. 它的药理基因特征允许方便的剂量,通常每天三次进行. 临床研究表明它能有效降低血清的发酵水平,改善心脏铁的过量,从而成为铁化疗程的有价值的治疗选择.

结构式图片

相似化合物

50700-61-3 76015-11-7 1346601-82-8

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合成工艺路线路线简述

  • 合成目标产物 Deferiprone 主要起始原料 3-Hydroxy-2-Methyl-4H-Pyran-4-One
  • (文献来源)合成步骤主要原料 3-Hydroxy-2-Methyl-4H-Pyran-4-One
3-(苄氧基)-2-甲基-4H-吡喃-4-酮置于palladium On Activated Charcoal 氢气体系中,用 甲醇,乙醇 用作溶剂,化学反应 24.0H,反应生成1,2-二甲基-3-羟基-4-吡啶酮
参考文献:3-Hydroxy-4-Pyrones As Precursors Of 4-Methoxy-3-Oxidopyridinium Ylides. An Expeditious Entry To Highly Substituted 8-Azabicyclo[3.2.1]octanes
标题:3-Hydroxy-4-Pyrones As Precursors Of 4-Methoxy-3-Oxidopyridinium Ylides. An Expeditious Entry To Highly Substituted 8-Azabicyclo[3.2.1]octanes
摘要:3-Hydroxy-4-Pyridones,Which Are Easily Prepared From Commercially Available 3-Hydroxy-4-Pyrones,Can Be Readily Transformed Into 4-Methoxy-3-Oxidopyridinium Ylides By Treatment With Methyl Trifluoromethanesulfonate And Subsequent Deprotonation With A Non-Nucleophilic Base. These Ylides Are Capable Of Undergoing Cycloaddition To Several Electron-Deficient Alkenes,Thus Allowing The Synthesis Of Highly Functionalized Azabicyclo[3.2,1]octane Moieties. The Rich Substitution Patterns Of These Frameworks Might Allow Their Divergent Conversion To A Variety Of Natural And Non-Natural Tropane Alkaloids.
Doi:10.1021/jo960854V

海关参考信息

专利信息


专利号:US-12264143-B2
优先权日:2020-12-17
标 题:Synthesis of cannabinoids and cannabinoid precursors, and related compounds, formulations, and methods of use
发明人:SAMMIS GLENN M; ROGGEN MARKUS
权利人:NALU BIO INC
摘要:Methods are provided for the synthesis of cannabinoids, including cannabidiol (CBD), cannabinol (CBN), cannabichromene (CBC), cannabidiolic acid (CBDA), cannabigerol (CBG), cannabigerolic acid (CBGA), cannabidivarin (CBDV), cannabidibutol (CBD-C4), dihydrocannabidiol (DCBD), tetrahydrocannabivarin (THCV), analogs thereof, and precursors to the foregoing. One method employs phloroglucinol or a phloroglucinol analog as a starting material. The syntheses are stereospecific, efficient, selective, and cost-effective, with little or no potential for generation of THC ((−)-trans-Δ9-tetrahydro-cannabinol) or any other psychoactive side product. Telescoped syntheses are also provided, as are new cannabinoids, pharmaceutical formulations, and methods of use.

专利号:US-7576234-B2
优先权日:2002-05-15
标题 :Synthesis of 2-alkyl amino acids
发明人:CHORGHADE MUKUND S; GURJAR MUKUND K; MOHAPATRA DEBENDRA K
权利人:GENZYME CORP
摘要:Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.

专利号:US-2022298522-A1
优先权日:2019-07-30
标 题:Methods of controlling cannabinoid synthesis in plants or cells and plants and cells produced thereby
发明人:FLAISHMAN MOSHE ARIE; SHAFRAN-TOMER HADAS; COHEN PEER REUT; COHEN ODED
权利人:THE STATE OF ISRAEL MINISTRY OF AGRICULTURE & RURAL DEVELOPMENT AGRICULTURAL RES ORGANIZATION
摘要:A method of controlling cannabinoid synthesis in a cell or plant or plant part comprising same is provided. The method comprising modulating expression in the cell of at least one polypeptide comprising an amino acid sequence at least 95% identical to SEQ ID NO: 1-15 and 18-86, the polypeptide modulating cannabinoid synthesis, thereby controlling cannabinoid synthesis in the cell. Also provided are methods of producing cannabinoids and selecting plants producing cannabinoids of interest.

专利号:US-9174846-B2
优先权日:2009-09-18
标题 :Ferric phosphate and methods of preparation thereof
发明人:BECK LARRY W; SOLTANI MAHROKH; WANG LIYA
权利人:BECK LARRY W; SOLTANI MAHROKH; WANG LIYA; A123 SYSTEMS LLC
摘要:High-purity crystalline ferric phosphate material with desirable characteristics for use in synthesis of nano-sized LFP cathode material are described. The ferric phosphate dihydrate material has as disclosed herein has a molar ratio of phosphorous to iron is from about 1.001 to about 1.05, a surface area of from about 25 m 2 /g to about 65 m 2 /g, and is substantially free of metallic or magnetic impurities. Methods of synthesizing high-purity crystalline ferric phosphate material with desirable characteristics for use in synthesis of nano-sized LFP cathode material are also described. In some embodiments, one or more magnetic traps are used during the reaction process and/or after the formation of the final product to remove magnetic impurities. In some embodiments, a synthetic method of ferric phosphate using multiple steps is described, wherein the intermediate of the synthesis is isolated and purified to improve the purity of the ferric phosphate material. In some embodiments, an iron compound is added to an aqueous solution of phosphoric acid. The solution pH and temperature are controlled to ensure the complete dissolution of the iron compound. The desired iron phosphate crystalline material can be obtained with high purity and high crystalline phase purity by controlling the pH and temperature of the solution.

专利号:US-6177409-B1
优先权日:1996-07-05
标 题 :Method for the site specific synthesis of novel 3-hydroxypyridin-4(1H)ons derivatives from aminomonosaccharides or aminoitols, products obtained by this method and their applications
发明人:VANLEMMENS PIERRE PAUL; POSTEL DENIS GHISLAIN; GERMAIN PIERIG EMMANUEL; JULIEN RENE JEAN-MARIE; PETIT JEAN-PIERRE CONSTANT; RONCO GINO LINO; VILLA PIERRE JOSEPH
权利人:INST BIOCHIMICO PAVESE PHARMA
摘要:Process for regiospecific preparation of new 3-hydroxypyridine-4(1H)-one derivatives starting from monosaccharides or itols of general formula:in which R represents a radical, either saturated or not, branched or not, having carbon-atom groups, and having hetero-atoms or not, and Sub represents a saccharide derivative or an itol, either cyclic not, protected or not, the hydrocarbon skeleton of which is bound to the nitrogen atom of the pyridinone either directly or by the intermediary of a spacing group. The present invention is characterized in that the process comprises a first step of protection of the 3-hydroxy group of the pyranone derivative, a second basocatalyzed step of substitution of the intracyclic oxygen atom of the pyranone by the nitrogen atom of the amine function of the amino monosaccharide or amino itol, and a third step of de-protection of the 3-OH group of the pyridinone cycle and possibly of the OH groups of the glucide or itol residue. It also regards the products obtained by this process, as well as their applications, namely as medicaments for the treatment of toxic overloads of FeIII.

专利号:WO-2024064745-A1
优先权日:2022-09-21
标 题:Synthesis of reldesemtiv
发明人:PETERSON MATTHEW W; LU QING; MORGAN BRADLEY P; ASHCRAFT LUKE W; ANDERSEN DENISE
权利人:CYTOKINETICS INC
摘要:Provided herein is a process for the preparation of reldesemtiv and salts thereof. Also provided herein are intermediates used in this process and their preparation.
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去铁酮Deferiprone
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主要参考文献


1: Fisher SA, Brunskill SJ, Doree C, Chowdhury O, Gooding S, Roberts DJ. Oral deferiprone for iron chelation in people with thalassaemia. Cochrane Database Syst Rev. 2013 Aug 21;8:CD004839. doi: 10.1002/14651858.CD004839.pub3. Review. doi: 10.1111/jnc.12300. Review. Review. doi: 10.3109/03630269.2010.484791. Review. doi: 10.3109/03630260903346924. Review. Review. doi: 10.1007/s10067-008-0969-y. Epub 2008 Jul 29. Review. doi: 10.1080/03630260701726533. Review.

合成参考文献


参考文献:10.1007/bf03346643
摘要:Poggi M, Pascucci C, Monti S, Pugliese P, Lauri C, Amodeo G, Girelli G, Toscano V. Prevalence of growth hormone deficiency in adult polytransfused β-thalassemia patients and correlation with transfusional and chelation parameters. Journal of Endocrinological Investigation. 2010 Feb 15;33(8):534–8. doi: 10.1007/bf03346643.
摘要:Sleem GA, Al-Zakwani IS, Almuslahi M. Hypoparathyroidism in adult patients with Beta-thalassemia major. Sultan Qaboos Univ Med J. 2007 Dec;7(3):215–8.
参考文献:10.2147/clep.s12502
摘要:Kriengkauykiat J, Ito JI, Dadwal SS. Epidemiology and treatment approaches in management of invasive fungal infections. Clin Epidemiol. 2011;3():175–91.
参考文献:10.4103/0974-1208.82369
摘要:Gude D. To 'umbrella' the gonads in transfusion rain. J Hum Reprod Sci. 2011 Jan;4(1):60–1.
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