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Idebenone, QSA-10, A-68500, CV-2619, Cerestabon, Mnesis, Avan

艾地苯醌Chemical Name: 2,3-Dimethoxy-5-methyl-6-(10'-hydroxydecyl)-1,4-benzoquinone
CAS No. 58186-27-9
项目整合开发状态: Launched-1986
项目研究机构: Takeda (Originator), TAP (Originator), Seber (Licensee)
合成路线:The radical alkylation of 2,3-dimethoxy-5-methylbenzoquinone (I) with bis(11-acetoxyundecanoyl)peroxide (II) at 85-90 C gives 2,3-dimethoxy-5-methyl-6-(10-acetoxydecyl)benzoquinone (III),which is hydrolyzed with concentrated HCl in methanol.
📌 参考资料/链接:
参考文献标题:Method of producing quinone derivatives
文献作者:Watanabe,M.; Imada,I.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0058057; JP 57131735; US 4831265

📄 详细内容


合成路线:The Friedel-Kraft condensation of 3,4,5-trimethoxytoluene (I) with ethyl 9-chloroformylnonanoate (II) by means of AlCl3 in nitrobenzene gives 9-(2-hydroxy-3,4-dimethoxy-6-methylbenzoyl)nonanoic acid (III),which is reduced with Zn in refluxing aqueous HCl yielding 10-(2-hydroxy-3,4-dimethoxy-6-methylphenyl)decanoic acid (IV).The oxidation of (IV) with potassium nitrosodisulfonate in water-acetone affords 2,3-dimethoxy-5-methyl-6-(9-carboxynonyl)benzoquinone (V),which is esterified with ethanol HCl to the corresponding ethyl ester (VI).Finally,this compound is reduced with LiAlH4 in ether.

参考文献标题:Aralkyl carboxylic acid compounds
文献作者:Morimoto,H.; Imada,I.; Watanabe,M.; Kawada,M.(Takeda Chemical Industries,Ltd.)
参考来源:BE 0828622; DE 2519730; FR 2269333; FR 2293194; JP 50148325; US 4139545; US 4525361


合成路线:The Friedel-Kraft condensation of 3,4,5-trimethoxytoluene (I) with ethyl 9-chloroformylnonanoate (II) by means of AlCl3 in nitrobenzene gives 9-(2-hydroxy-3,4-dimethoxy-6-methylbenzoyl)nonanoic acid (III),which is reduced with Zn in refluxing aqueous HCl yielding 10-(2-hydroxy-3,4-dimethoxy-6-methylphenyl)decanoic acid (IV).The oxidation of (IV) with potassium nitrosodisulfonate in water-acetone affords 2,3-dimethoxy-5-methyl-6-(9-carboxynonyl)benzoquinone (V),which is esterified with ethanol HCl to the corresponding ethyl ester (VI).Finally,this compound is reduced with LiAlH4 in ether.

参考文献标题:Method for therapy of ischemic disease
文献作者:Imada,I.; Nagaoka,A.; Hirata,M.(Takeda Chemical Industries,Ltd.)
参考来源:DE 3049039; EP 0031727; JP 56097223; US 4436753


合成路线:The Friedel-Kraft condensation of 3,4,5-trimethoxytoluene (I) with ethyl 9-chloroformylnonanoate (II) by means of AlCl3 in nitrobenzene gives 9-(2-hydroxy-3,4-dimethoxy-6-methylbenzoyl)nonanoic acid (III),which is reduced with Zn in refluxing aqueous HCl yielding 10-(2-hydroxy-3,4-dimethoxy-6-methylphenyl)decanoic acid (IV).The oxidation of (IV) with potassium nitrosodisulfonate in water-acetone affords 2,3-dimethoxy-5-methyl-6-(9-carboxynonyl)benzoquinone (V),which is esterified with ethanol HCl to the corresponding ethyl ester (VI).Finally,this compound is reduced with LiAlH4 in ether.
参考文献标题:CV-2619
文献作者:Serradell,M.N.; Castar,J.; Blancafort,P.
参考来源:Drugs Fut 1983,8(7),583


产品链接: CAS No. 58186-27-9››