CAS: 1222-57-7; 2-(4-(Methylsulfonyl)Phenyl)Imidazo[1,2-A]Pyridine

该化合物是一种化学化合物,属于伊米达佐尔衍生物的类别,主要因其药理特性而得到承认,特别是抗口炎和潜在的抗炎剂.Zolimidine展示了一个以其与生物系统互动的能力为特征的结构,该机环以其与生物系统互动的能力而著称,特别是在调制三聚胺受体方面.该机组通常在各种配方中施用,其功效经常在过敏反应和相关条件下进行评估.从物理特性来看,Zolimidine一般在室内温度下是固态的,有机溶剂中溶解,便于其用于制药用途.安全性和毒性特征是其使用的基本考虑因素,与任何药用活性物质一样.

结构式图片

上下游产品

2-(4-甲硫基苯基)咪唑并[1,2-A]吡啶 2-(4-(Methylthio)Phenyl)Imidazo[1,2-A]Pyridine 2076-70-2
2-(4-溴苯基)咪唑并[1,2-A]吡啶 2-(4-Bromophenyl)Imidazo[1,2-A]Pyridine 34658-66-7
2-(4-Iodophenyl)Imidazo[1,2-A]Pyridine 214958-27-7

合成工艺路线路线简述

    📜茴香硫醚置于aluminum (III) Chloride,N-溴代丁二酰亚胺(Nbs),水,碳酸氢钠,对甲苯磺酸体系中,用 1,4-二氧六环,乙醇 用作溶剂,化学反应 26.0H,反应生成佐利米定
    参考文献:新型咪唑并[1,2-A]吡啶衍生物作为选择性cox-2抑制剂的设计,合成和生物学评价
    标题:新型咪唑并[1,2-A]吡啶衍生物作为选择性cox-2抑制剂的设计,合成和生物学评价
    摘要:设计并合成了三个新系列的含甲基磺酰基咪唑并[1,2-A ]吡啶8A-D,9A-D和10A-D.使用光谱和元素分析对这些新化合物的化学结构进行了表征.除了体内抗炎活性外,还测试了合成的衍生物抑制 Cox-1 和 Cox-2 同工酶的能力.吡唑啉衍生物 9A 在所有化合物中对 Cox-2 同工酶的选择性指数最高(si = 39),几乎是塞来昔布(si = 13.76)的三倍,具有非常好的体内抗炎活性(水肿抑制百分比 = 11.16-32.64).化合物 10C 对 Cox-2 同工酶的抑制活性最高 (Ic 50 = 1.06 µm),它是最有效的抗炎衍生物(水肿抑制百分比 = 15.04-42.35),Ed 50值为 69.46 µmol/kg,比塞来昔布(ed 50 = 104.88 µmol)强大约一倍半/公斤).此外,最有效的抗炎化合物 9A,9D,10C 和 10D 进行了溃疡倾向和组织病理学检查.化合物
    Doi:10.1016/j.Molstruc.2021.131652

    海关参考信息

    专利信息


    专利号:US-2025101045-A1
    优先权日:2022-01-18
    标题:Synthesis of boron-containing amidoxime reagents and their application to synthesize functionalized oxadiazole and quinazolinone derivatives
    发明人:DAS BHASKAR
    权利人:LONG ISLAND UNIV
    摘要:The present disclosure is concerned with borylated amidoximes useful in the synthesis of biologically relevant drug-like molecules, including functionalized oxadizole and quinazolinone derivatives. Also disclosed are methods of making borylated amidoximes, methods of making functionalized oxadiazole and quinazolinone compounds using the amidoximes, and functionalized oxadiazole and quinazolinone compounds prepared from borylated amidoximes. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    专利号:US-4469701-A
    优先权日:1983-06-23
    标题 :Pyrrolid-3-en-2-ones and pharmaceutical methods of use thereof
    发明人:DEBAUN JACK R; PALLOS FERENC M; MATSUMOTO KENT E; ROSS JOHN H
    权利人:STAUFFER CHEMICAL CO
    摘要:Novel compounds having the structural formula ##STR1## wherein R 1 and R 2 are independently selected from the group consisting of hydrogen, halo, alkyl, haloalkyl, thioalkyl, thiohaloalkyl, alkoxy, cyano and nitro are provided. The compounds have various pharmacological effects, including cardiotropic, hypoglycemic, hypocholesterolemic and/or antiulcerative effects in mammals. Methods of achieving these various pharmacological effects in mammals by administering the compounds thereto are provided. Pharmaceutical compositions and formulations including the compounds are provided along with methods of synthesis of the novel compounds.

    专利号:WO-2023141114-A2
    优先权日:2022-01-18
    标 题:Synthesis of boron-containing amidoxime reagents and their application to synthesize functionalized oxadiazole and quinazolinone derivatives

    专利号:AU-2023208727-A1
    优先权日:2022-01-18
    标题:Synthesis of boron-containing amidoxime reagents and their application to synthesize functionalized oxadiazole and quinazolinone derivatives

    专利号:EP-4466275-A2
    优先权日:2022-01-18
    标 题 :Synthesis of boron-containing amidoxime reagents and their application to synthesize functionalized oxadiazole and quinazolinone derivatives

    专利号:US-2020335181-A1
    优先权日:2018-01-09
    标题:Digital reactionware
    发明人:CRONIN LEROY
    权利人:UNIV GLASGOW COURT
    摘要:The invention provides a method for digitising a method of synthesis. The method includes the steps of identifying a method of synthesis for a target product; (ii) establishing a process sequence for that method, which process sequence is a collection of chemical and/or physical steps within the method of synthesis; and subsequently (iii) translating the process sequence to a digital model of the method of synthesis, which digital model comprises a digital description of the chemical and/or physical steps within the method of synthesis.

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    主要参考文献


    1: Narayan A, Patel S, Baile SB, Jain S, Sharma S. Imidazo[1,2-A]Pyridine: Potent Biological Activity, SAR and Docking Investigations (2017-2022). Infect Disord Drug Targets. 2024;24(8):e200324228067. doi: 10.2174/0118715265274067240223040333. 25(6):e202300824. doi: 10.1002/cbic.202300824. Epub 2024 Feb 20. 24(9):1111-1123. doi: 10.2174/1566524023666230726160056. 26(6):106834. doi: 10.1016/j.isci.2023.106834.
    5: Tali JA, Shankar R. Ru(II)-Catalyzed Synthesis of Fused Imidazo[1,2-a]pyridine-chromenones and Methylene-Tethered Bis- imidazo[1,2-a]pyridines and Regioselective O-Acetoxylation of Imidazo[1,2-a]pyridines. Org Lett. 2023 May 12;25(18):3200-3205. doi: 10.1021/acs.orglett.3c00578. Epub 2023 May 4. 14(21):1491-1494. doi: 10.4155/fmc-2022-0148. Epub 2022 Oct 3. 50(47):17515-17523. doi: 10.1039/d1dt02985a. 19(43):9401-9406. doi: 10.1039/d1ob01683k. 23(19):7370-7375. doi: 10.1021/acs.orglett.1c02536. Epub 2021 Sep 20. 5(22):13333-13343. doi: 10.1021/acsomega.0c01478.
    11: Samanta SK, Bera MK. Iodine mediated oxidative cross coupling of 2-aminopyridine and aromatic terminal alkyne: a practical route to imidazo[1,2-a]pyridine derivatives. Org Biomol Chem. 2019 Jul 14;17(26):6441-6449. doi: 10.1039/c9ob00812h. Epub 2019 Jun 17. Erratum in: Org Biomol Chem. 2019 Aug 7;17(31):7425. doi: 10.1039/c9ob90125f. 20(16):4858-4861. doi: 10.1021/acs.orglett.8b02003. Epub 2018 Aug 7. 17(2):238-250. doi: 10.2174/1568026616666160530153233. 20(3):659-66. doi: 10.1007/s11030-016-9666-y. Epub 2016 Mar 14. 78(24):12494-504. doi: 10.1021/jo402134x. Epub 2013 Dec 3. 48(90):11073-5. doi: 10.1039/c2cc35927h. Epub 2012 Sep 27. 39(11):2937-43. doi: 10.1248/cpb.39.2937. 60(4):761-7. Italian.

    合成参考文献


    参考文献:10.1107/s1600536811017077
    摘要:Dahmani S, Kandri Rodi Y, Luis SV, Essassi el M, El Ammari L. Ethyl 8-amino-6-bromoimidazo[1,2-a]pyridine-2-carb-oxy-late. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1390.
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