CAS: 4965-26-8; 5-Nitrobenzo[b]Thiophene

该化合物是一种硝基替代苯并苯衍生物,主要用作有机合成和制药研究的中间体,其结构以一个附属于苯并氧基的硝基集团为主,增强了电子和核循环替代反应的回活动性,使其对构建复杂的杂交环化合物具有价值;该化合物在标准条件下具有稳定性,在普通有机溶剂中可溶解,便于其用于多种合成用途;其硝基苯衍生物组还作为进一步功能化的前体,能够合成阿明斯,阿明斯和其他衍生物.这种多功能性使5-Nitrobenzothiophene成为医药化学和物质科学的有用建筑块.

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上下游产品

5-nitrobenzo[b]thiophene-2-carboxylic acid (4-nitro-phenylsulfanyl)-acetaldehyde dimethylacetal (1E,3Z)-3-(4-methanesulfonyl-2-nitrobuta-1,3-dien-1-yl)thiophene ethyl 5-nitro-2-benzo[b]thiophenecarboxylate 5-aminobenzo[b]thiophene 3-bromo-5-nitrobenzo[b]thiophene 1-(5-benzo[b]thiophenyl)piperazine benzo[b]thiophen-5-ol

合成工艺路线路线简述

    2-氯-5-硝基苯甲醛置于喹啉,水,铜,Potassium Carbonate,Sodium Hydroxide体系中,用 甲醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 8.0H,反应生成 5-硝基苯并噻吩
    参考文献:闭环策略导致有效的ripk3抑制剂
    标题:闭环策略导致有效的ripk3抑制剂
    摘要:坏死性坏死是调节坏死性细胞死亡的一种形式,与胱天蛋白酶无关.受体相互作用蛋白激酶3(ripk3)已被确定为坏死病的关键调节剂,并已被提议作为治疗坏死病相关疾病的潜在治疗靶标.在本报告中,我们描述了一系列新型ripk3抑制剂的设计,合成和评估.铅化合物38 在阻断tnf-α,Smac模拟物和z-Vad(tsz)诱导的ht-29细胞死亡中表现出强大的活性(ec 50 = 0.42μm).机理研究表明,化合物38与ripk3具有高亲和力(k D = 7.1 Nm)结合,并在adp-Glo功能测定中抑制了ripk3激酶活性.另外,复合38显示出优于另一种坏死性调节剂ripk1(k D = 6000 Nm)的选择性.此外,化合物38表现出优异的体外安全性,对cyp同工酶和herg钾通道的抑制作用最小.最后,化合物38在tnfα诱导的全身性炎症反应综合征模型中有效阻断了小鼠的体温过低和死亡.
    DOI:10.1016/j.Ejmech.2021.113327

    专利信息


    专利号:US-RE35279-E
    优先权日:1987-08-28
    标题:Hydantoin derivatives
    发明人:MOCHIDA EI; MURAKAMI KIMIHIRO; KATO KAZUO; KATO KATSUAKI; OKUDA JUN; MIWA ICHITOMO
    权利人:MOCHIDA PHARM CO LTD
    摘要:The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives. The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton. The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.

    专利号:US-5202339-A
    优先权日:1987-08-28
    标题:Hydantoin derivatives
    发明人:MOCHIDA EI; MURAKAMI KIMIHIRO; KATO KAZUO; KATO KATSUAKI; OKUDA JUN; MIWA ICHITOMO
    权利人:MOCHIDA PHARM CO LTD
    摘要:The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives and pharmaceutical compositions containing at least one of hydantoin derivatives as hypoglycemic as well as hypolipidemic agents. The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton. The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites. The compounds of the present invention represent a satisfactory hypoglycemic as well as hypolipidemic activity. These compounds are extremely useful for the treatment and/or prevention of diabetes mellitus with or without hyperlipidemia. It is indicated that the compounds of the present invention are useful for the treatment and/or prevention of diabetic complications such as somatic or autonomic neuropathy, cataract, retinopathy, nephropathy or microangiopathy. It is also indicated that the compounds of the present invention are useful for the treatment and/or prevention of hyperlipidemia.

    专利号:EP-0355827-B1
    优先权日:1988-08-24
    标 题:Hydantoin derivatives
    发明人:MOCHIDA EI; MURAKAMI KIMIHIRO; KATO KAZUO; KATO KATSUAKI; OKUDA JUN; MIWA ICHITOMO A
    权利人:MOCHIDA PHARM CO LTD
    摘要:The present invention relates to hydantoin derivatives, represented by the formula (I): and non-toxic salts, solvates and solvates of non-toxic salts thereof; wherein q represents a mono- or a fused heterocyclic group which may be substituted by one or more substituents which are same or different and selected from a group consisting of a halogen atom, an alkyl group, a nitro group, a cyano group, an optionally protected carboxy group, an optionally protected carboxymethyl group, a halogenated alkyl group, an alkylthio group, an alkylcarbonyl group, an alkoxy group, an alkylsulfinyl group, an alkylsulfonyl group, an optionally protected hydroxy group, an optionally protected amino group, a carbamoyl group and a phenyl group, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and intermediate compounds in the synthesis of said hydantoin derivatives.

    专利号:CN-116554087-B
    优先权日:2023-05-15
    标题 :A method for light-induced synthesis of carbazole compounds

    专利号:CN-114656389-B
    优先权日:2022-04-27
    标题 :Synthesis method of 1-phenylpyrrolidine

    专利号:CN-114507252-A
    优先权日:2022-02-21
    标题:Synthesis method of novel aryl silane compound
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    合成参考文献


    摘要:Rück-Braun, K.; Priewisch, B., Science of Synthesis, (2007) 31, 1336.
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