CAS: 139162-43-9; N-(5,5,8,8-Tetramethyl-5,6,7,8-Tetrahydronaphthalen-2-yl)Acetamide

上下游产品

2,5-dichloro-2,5-dimethyl hexane Acetanilid 2,5-dimethyl-2,5-hexanediolN-phenyl-5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalene-2,3-diamine N-methyl-N-phenyl-5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalene-2,3-diamine (5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-nitro-2-naphthyl)phenylamine Methyl-phenyl-(5,5,8,8-tetramethyl-3-nitro-5,6,7,8-tetrahydro-naphthalen-2-yl)-amine

2,5-二甲基-2,5-己二醇置于盐酸,Aluminum (III) Chloride体系中,用 二氯甲烷,水 用作溶剂,化学反应 4.0H,反应生成N-(5,5,8,8-四甲基-5,6,7,8-四氢-2-萘)乙酰胺 (他米巴罗汀)
参考文献:生物活性分子发现中的古巴范式:进一步的范围,局限性和环辛酸酯的互补性.
标题:生物活性分子发现中的古巴范式:进一步的范围,局限性和环辛酸酯的互补性.
摘要:在广泛的研究中进一步探索了古巴苯环生物立体异构体范式,涵盖了广泛的药物和农用化学模板,其中包括抗生素(头孢克洛,青霉素g)和抗组胺药(苯海拉明),平滑肌松弛剂(金银花),麻醉剂(氯胺酮) ),农药杀虫剂(triflumuron),抗寄生虫药(苯并硝唑)和抗癌剂(他米巴罗汀).这项研究从合成相容性和物理性质匹配两方面突出了将古巴人纳入生物活性分子发现的范围和局限性.在chagas病抗寄生虫苯并硝唑的情况下,Cuban保持了生物等排作用,尽管在抗癌药(他米巴罗汀)方面活性较低.发现应用环辛酸酯(cot)(生物)基序补体相对于苯母体可优化苯硝唑,并在他米巴罗汀的情况下相对于古巴类似物具有增强的抗癌活性.像所有生物等排体,支架和生物基序一样,也存在局限性(例如合成实现),在此使用失败的示例对它们进行了特别强调.迄今为止,由我们小组准备的所有模板的摘要均经过了生物学评估,这强烈支持以下观点:古巴是生
Doi:10.1039/c9Ob01238A

专利信息

专利号:US-5214202-A
优先权日:1990-03-20
标 题:Method for preparing benzoic acid derivatives
发明人：HAMADA YOSHINORI; YAMADA ISAMU; UENAKA MASAAKI; SAKATA TERUO
权利人:SHIONOGI & CO
摘要:This invention relates to a synthesis method favorable for the industrial production of a benzoic acid derivative having a retinoid activity of the general formula: ##STR1## wherein the derivative can be obtained by a simple procedure in safety with high yield. n Specifically, this invention relates to a synthesis method characterized in that only one vessel is needed for several reactions in the different steps of subjecting acetanilide as a starting material, which is readily available and safe to handle, to Friedel-Crafts reaction with 2,5-dimethyl-2,5-dichlorohexane; subjecting the thus obtained compound to acyl exchange reaction with monomethyl ester terephthalic chloride, followed by hydrolysis; and recrystallizing from a mixture of methanol and water. n Moreover, the crystals in novel form obtained by the synthesis method of this invention are suitable for formulation, because the amount of solvents remaining therein after recrystallization is small and the grain size thereof is uniform.