CAS: 2148-57-4; 4,7-Dichloroquinazoline

该化合物是一种卤化的五氯二烯衍生物,广泛用作有机合成和制药研究的多用途中间体,其主要优点包括:由于在4和7个位置存在两个氯替代体,因此具有高度的再活性,从而能够为进一步实现功能化而进行有效的核循环替代反应;该化合物是发展生物活性分子,特别是合成动脉抑制剂和其他三环化合物的宝贵构件;其稳定性和明确界定的晶体结构有利于实验室环境的精确处理;二氯化五氯二苯核心也为药用化学的修改提供了潜力,使它成为用于药物发现应用的有用的手杖.

结构式图片

欧盟法规

C&L通报

上下游产品

7-氯-4(3H)-喹唑啉酮 7-Chloro-3,4-Dihydroquinazolin-4-One 31374-18-2

合成工艺路线路线简述

  • 合成目标产物 4,7-Dichloroquinazoline 主要起始原料 7-Chloro-4-Quinazolinol
  • (文献来源)合成步骤主要原料 7-Chloro-4-Quinazolinol
📜7-氯-4(3H)-喹唑啉酮置于氯化亚砜体系中,化学反应生成4,7-二氯喹唑啉
参考文献:通过基于结构的方法发现新型登革热病毒进入抑制剂
标题:通过基于结构的方法发现新型登革热病毒进入抑制剂
摘要:登革热是一种由蚊子传播的病毒,近年来已成为全球主要的公共卫生问题.但是,目前对登革热疾病的治疗仅是支持性治疗,尚无特异性抗病毒药可用于控制感染.因此,最需要安全有效的抗病毒药物.登革热病毒(denv)进入宿主细胞的过程是由其主要包膜蛋白e介导的.E蛋白的晶体结构揭示了位于结构域i和ii之间铰链区的去污剂n-辛基-β-D-葡萄糖苷(β-Og)占据的疏水口袋,这对于低ph触发很重要融合所需的构象重排.因此,E蛋白是开发抗病毒剂的有吸引力的靶标.在这项工作中,我们进行了基于前期对接的虚拟筛选,以鉴定可能与β-Og结合位点结合的小分子.鉴定出了23种结构上不同的化合物,其中两个在低微摩尔范围内的ec 50值.特别地,化合物2(ec 50 = 3.1μm)显示出显着的抗病毒活性并具有非常好的治疗指数.使用分子动力学模拟来尝试表征2与蛋白质e的相互作用,从而为将来的配体优化工作铺平了道路.这些研究突
Doi:10.1016/j.Bmcl.2017.06.049

海关参考信息

专利信息


专利号:US-7825244-B2
优先权日:2005-06-10
标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis
发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG
权利人:JANSSEN PHARMACEUTICA NV
摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.

专利号:US-11225655-B2
优先权日:2010-04-16
标题:Bi-functional complexes and methods for making and using such complexes
发明人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK
权利人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK; NUEVOLUTION AS
摘要:The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.

专利号:US-2007021436-A1
优先权日:2005-06-10
标 题 :Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis

专利号:CA-2611219-A1
优先权日:2005-06-10
标题 :Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators and related methods of synthesis

专利号:AU-2006258056-A1
优先权日:2005-06-10
标 题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators and related methods of synthesis

专利号:KR-20080033234-A
优先权日:2005-06-10
标 题 :Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators and related methods of synthesis

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品牌试剂参考报价(招募中)

📌 第三方产品分析报告

✅ COA系统入驻 | 共享模式

合成参考文献


参考文献:10.1134/s1070363220120294
摘要:Abdulwahab MK, Dzulkeflee R, Han TK, Ruslan RA, Leong KH, Heh CH, Ariffin A. Synthesis, In Vitro Antiproliferative Activity, and In Silico Studies of New Anilinoquinazoline Derivatives as Potential AntitumorAgents. Russian Journal of General Chemistry. 2020 Dec;90(12):2410–8. doi: 10.1134/s1070363220120294.
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