CAS: 55827-50-4; 1-(3,5-Dichlorophenyl)Piperazine

该化合物是一种化学化合物,用3,5-二氯苯基组替代了管子核心,这种结构在制药和农用化学研究中具有多功能性,特别是作为生物活性分子合成的中间体.它的二氯苯基能会提高亲脂性,有可能提高药物开发中膜的渗透性.该化合物的稳定性和定义明确的再活性使它适合选择性功能化,从而能够精确修改目标应用.它由于在结构上与主要药用植物相似,因此在对血清受体进行的研究中常用.高纯度能确保研究环境中的再生性,支持其在方法开发和机械研究中的使用.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

合成工艺路线路线简述

    3,5-二氯-1-溴苯置于tris-(Dibenzylideneacetone)Dipalladium(0),R-(+)-1,1'-联萘-2,2'-双二苯膦,三氟乙酸,Sodium T-Butanolate体系中,用 二氯甲烷,甲苯 作为反应溶剂,化学反应 15.0H,反应生成 1-(3,5-二氯苯基)哌嗪
    参考文献:具有混合结构的新型苯甘氨酰胺衍生物可作为新型广谱抗惊厥药的候选者
    标题:具有混合结构的新型苯甘氨酰胺衍生物可作为新型广谱抗惊厥药的候选者
    摘要:在本研究中,应用集中的组合化学方法将众所周知的 Trpv1 拮抗剂的结构片段与我们小组先前发现的强效抗惊厥先导化合物ka-104合并.因此,在体内和体外试验中设计,合成和表征了一系列 22 种原始化合物.获得的化合物在最大电击 (Mes) 测试和 6 Hz 癫痫模型(使用 32 和 44 Ma 电流强度)中显示出强大的体内抗癫痫活性.最有效的化合物53和60显示出以下药理学特征:Ed 50 = 89.7 Mg/kg (Mes),Ed 50 = 29.9 Mg/kg (6 Hz,32 Ma),Ed 50= 68.0 Mg/kg (6 Hz,44 Ma),Ed 50 = 73.6 Mg/kg (Mes),Ed 50 = 24.6 Mg/kg (6 Hz,32 Ma),Ed 50 = 56.3 Mg/kg (6赫兹,44毫安),分别.此外,53和60对iv Ptz 癫痫发作阈值有效,
    DOI:10.3390/cells11121862

    海关参考信息

    专利信息


    专利号:US-2005019747-A1
    优先权日:2002-08-07
    标 题 :Nanoliter-scale synthesis of arrayed biomaterials and screening thereof
    发明人:ANDERSON DANIEL G; LEVENBERG SHULAMIT; LANGER ROBERT S
    摘要:A method of screening cell-polymer interactions. The method includes depositing monomers as a plurality of discrete elements on a substrate, causing the deposited monomers to polymerize, thereby creating an array of discrete polymer elements on the substrate, incubating the substrate in a cell-containing culture medium, and characterizing a predetermined cell behavior on each polymer element.

    专利号:US-10995078-B2
    优先权日:2013-03-13
    标 题:Compounds and compositions for inhibition of FASN
    发明人:BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J
    权利人:FORMA THERAPEUTICS INC
    摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:

    专利号:CA-2539670-A1
    优先权日:2003-09-15
    标 题:Nanoliter-scale synthesis of arrayed biomaterials and screening thereof

    专利号:WO-2005028619-A2
    优先权日:2003-09-15
    标题:Nanoliter-scale synthesis of arrayed biomaterials and screening thereof

    专利号:US-6552018-B1
    优先权日:1997-01-27
    标 题:Pyrazole derivatives
    发明人:EJIMA AKIO; OHSUKI SATORU; OHKI HITOSHI; NAITO HIROYUKI
    权利人:DAIICHI SEIYAKU CO
    摘要:The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): n wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: n These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)- 1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.

    专利号:US-9676721-B2
    优先权日:2010-09-03
    标题 :Compounds and compositions for the inhibition of NAMPT
    发明人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG
    权利人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC
    摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
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    合成参考文献


    参考文献:10.1007/s11094-020-02119-9
    摘要:Özdemir A, Turanli S, Çalişkan B, Arka M, Banoglu E. Evaluation of Cytotoxic Activity of New Benzimidazole-Piperazine Hybrids Against Human MCF-7 and A549 Cancer Cells. Pharmaceutical Chemistry Journal. 2020 Feb 22;53(11):1036–46. doi: 10.1007/s11094-020-02119-9.
    参考文献:10.1007/s13738-015-0762-1
    摘要:Mistry B, Keum Y, Noorzai R, Gansukh E, Kim DH. Synthesis of piperazine based N-Mannich bases of berberine and their antioxidant and anticancer evaluations. Journal of the Iranian Chemical Society. 2015 Oct 27;13(3):531–9. doi: 10.1007/s13738-015-0762-1.
    参考文献:10.1007/s00044-022-02873-3
    摘要:Blass BE, Chen P, Taylor M, Griffin SA, Gordon JC, Luedtke RR. Design, synthesis, and evaluation of functionalized 5-(4-arylpiperazin-1-yl)-N-quinolinyl-pentanamides as selective dopamine D3 receptor ligands. Medicinal Chemistry Research. 2022 Mar 23;31(5):749–61. doi: 10.1007/s00044-022-02873-3.
    参考文献:10.1007/s00044-021-02845-z
    摘要:Blass BE, Chen P, Taylor M, Griffin SA, Gordon JC, Luedtke RR. Synthesis and evaluation of cyclic diamino benzamide based D3 receptor ligands. Medicinal Chemistry Research. 2022 Feb 02;31(3):446–61. doi: 10.1007/s00044-021-02845-z.
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