CAS: 6082-66-2; 3,4,6-Trichloropyridazine

该化合物是一种氯化异环化合物,分子式为C4HCl3N2.它是一个有机合成的多用途中间体,特别是在制药,农用化学品和特殊化学品的准备方面.第3,4和6号阵地有三个活氯原子,允许选择性地发挥功能,使多种衍生物能够合成.它的高度纯度和稳定性使它适合精确的合成应用.该化合物通常用于核本体替代反应,交叉相交过程,以及作为更复杂的循环结构的建筑块.由于在某些条件下具有潜在的再活动性,需要适当的处理.

结构式图片

相似化合物

20074-67-3 14161-11-6 1677-80-1

欧盟法规

ECHA物质C&L通报

上下游产品

4-chloro-1,2-dihydro-pyridazine-3,6-dione 4-bromo-1,2-dihydropyridazine-3,6-dione 3,6-dichlorpyridazine pyridazine-3,4,6-triol 4,6-dichloro-2,3-dihydropyridazin-3-one 5,6-dichloro-2,3-dihydropyridazin-3-one H-pyridazin-4-one3,6-dichloro-1H-pyridazin-4-one 3,6-dichloropyridazin-4-amine

合成工艺路线路线简述

    溴代马来酸酐置于肼,三氯氧磷体系中,用 水 作为反应溶剂,化学反应 7.5H,以87%的收率获得产物3,4,6-三氯哒嗪
    参考文献:作为细菌iia型拓扑异构酶的有效抑制剂的新型三环类化合物(例如,Gsk945237)
    标题:作为细菌iia型拓扑异构酶的有效抑制剂的新型三环类化合物(例如,Gsk945237)
    摘要:在我们对nbti(新型ii型细菌拓扑异构酶抑制剂)抗菌剂的前导优化研究过程中,我们发现了一系列三环化合物,它们均显示出非常好的革兰氏阳性和革兰氏阴性效能.在这里,我们将讨论在本系列中研究的各种亚基,并报告对化合物1(gsk945237)的高级研究,该研究证明了非常好的pk和体内功效.
    DOI:10.1016/j.Bmcl.2016.03.106

    专利信息


    专利号:RU-2024517-C1
    优先权日:1988-12-06
    标 题:Method of synthesis of piperazinylalkyl-3-(2h)-pyridazinones or their pharmaceutically acceptable salts

    专利号:WO-2024256496-A1
    优先权日:2023-06-14
    标题 :[1,2,4]-triazolo[4,3-b]pyridazine derivatives useful as a medicament
    发明人:ELIE JONATHAN; GEORGE PASCAL; MIEGE FRÉDÉRIC; MEIJER LAURENT
    权利人:PERHA PHARMACEUTICALS
    摘要:The present invention relates to a compound of formula (I) or any of its pharmaceutically acceptable salt. The present invention further relates to a synthesis process for manufacturing compound of formula (I) or any of its pharmaceutically acceptable salts, comprising at least a step of reacting a compound of formula (II) with an amine of formula (IV) NHR5R6 for example in a molar ratio ranging from 1 to 20 eq, with respect to the compound of formula (II), in an aprotic solvent or without solvent or else in a protic solvent.

    专利号:US-12428395-B2
    优先权日:2019-08-01
    标题 :Heterocyclic compounds as kinase inhibitor and uses thereof
    发明人:PENDHARKAR DHANANJAY; RAMACHANDRAN SREEKANTH A; JADHAVAR PRADEEP S; PANPATIL DAYANAND; SAEED UZMA; KUMAR VIVEK; BIST DIPSHE
    权利人:SPEROGENIX THERAPEUTICS LTD
    摘要:The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (IA), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed.

    专利号:WO-2022162606-A1
    优先权日:2021-01-30
    标 题:Heterocyclic compounds as kinase inhibitor and uses thereof
    发明人:YAN ZHIYU; WANG XIAOHUI; LIU HANLAN; KHAN PASHA M; PANPATIL DAYANAND; PUJALA BRAHMAM; PENDHARKAR DHANANJAY; JADHAVAR PRADEEP S; SAEED UZMA; KUMAR VIVEK
    权利人:SPEROGENIX THERAPEUTICS LTD; INTEGRAL BIOSCIENCES PRIVATE LTD
    摘要:The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (J), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes such as cancer, idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed. Formula (J)
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    合成参考文献


    参考文献:10.1007/bf00779120
    摘要:Savitskaya NV, Gortinskaya TV, Nyrkova VG, Fedorova IN, Polezhaeva AI, Mashkovskii MD, Shchukina MN, Vlasova TV. Synthesis and pharmacological study of 5h-pyridazino[3,4-b]1,4-benzoxazines (3,4-diazaphenoxazines). Pharmaceutical Chemistry Journal. 1977 Jan;11(1):53–60. doi: 10.1007/bf00779120.
    参考文献:10.1007/bf00758030
    摘要:Savitskaya NV, Gortinskaya TV, Nyrkova VG, Fedorova IN, Polezhaeva AI, Mashkovskii MD, Shchukina MN. Synthesis of 5H-pyridazo[3,4-b]-1,4-benzoxazines (3,4-diazaphenoxazines). Pharmaceutical Chemistry Journal. 1976 Jul;10(7):868–72. doi: 10.1007/bf00758030.
    参考文献:10.1007/bf00772309
    摘要:Predvoditeleva GS, Kartseva TV, Shchukina MN. Pyridazinoquinoxalines. Pharmaceutical Chemistry Journal. 1973 May;7(5):278–81. doi: 10.1007/bf00772309.
    参考文献:10.1007/bf00771491
    摘要:Gortinskaya TV, Nyrkova VG, Savitskaya NV, Shchukina MN, Klimonova ZM, Potapova VG, Gorodetskii LS, Volzhina ON. Method of preparation of azaphene. Pharmaceutical Chemistry Journal. 1973 Jun;7(6):353–5. doi: 10.1007/bf00771491.
    参考文献:10.1007/978-3-642-02035-3_138
    摘要:Jolanki R. Chemists. 2012. In: Kanerva's Occupational Dermatology. : Springer Berlin Heidelberg; 2012.
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