(E)-4-bromopent-2-enoyl chloride

• 分子结构分类: 有机化合物 - 有机卤素化合物 - 酰卤
• 英文名称: (E)-4-bromopent-2-enoyl chloride
• 化学式: C₅H₆BrClO
• 分子量: 197.459
• InChiKey: BFQUBGDESCUNPP-NSCUHMNNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  8
• 可旋转键数：
  2
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  17.1
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  (E)-4-bromopent-2-enoyl chloride 在 盐酸 、 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 sodium carbonate 、 caesium carbonate 、 N,N-二异丙基乙胺 作用下， 以 2-甲基四氢呋喃 、 二氯甲烷 、 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 28.0h， 生成
  参考文献：
  名称：

  EP3889133

  摘要：

  公开号：
• 作为产物：
  描述：

  反式-2-戊烯酸 在 N-溴代丁二酰亚胺(NBS) 、 氯化亚砜 作用下， 以 四氯化碳 为溶剂， 反应 24.0h， 生成 (E)-4-bromopent-2-enoyl chloride
  参考文献：
  名称：

  EP3889133

  摘要：

  公开号：

文献信息

• [EN] N-HETEROARYL COMPOUNDS WITH CYCLIC BRIDGING UNIT FOR THE TREATMENT OF PARASITIC DISEASES<br/>[FR] COMPOSÉS N-HÉTÉROARYLÉS AYANT UNE UNITÉ PONTANTE CYCLIQUE POUR LE TRAITEMENT DE MALADIES PARASITAIRES
  申请人：INTERVET INT BV

  公开号：WO2012041872A1

  公开（公告）日：2012-04-05

  This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.

  这项发明涉及某些N-杂环芳基化合物，通常用作药物，更具体地用作动物药物。该药物可以优选用于治疗蠕虫感染和寄生虫病的治疗，例如由蠕虫感染引起的寄生虫病。该发明还涉及利用这些化合物制备药物和治疗方法，包括将这些化合物用于需要治疗的动物的给药。此外，该发明还涉及N-杂环芳基化合物的制备。此外，该发明还涉及包含这些化合物的药物组合物和试剂盒。
• N-heteroaryl compounds with cyclic bridging unit for the treatment of parasitic diseases
  申请人：Berger Michael

  公开号：US08883791B2

  公开（公告）日：2014-11-11

  This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.

  本发明涉及某些N-杂环芳基化合物，通常作为药物使用，更具体地作为动物药物。该药物可优选用于治疗蠕虫感染和寄生虫病的治疗，例如由蠕虫感染引起的寄生虫病。本发明还涉及使用这些化合物制备药物和治疗方法，包括向需要治疗的动物施用这些化合物。本发明还涉及制备N-杂环芳基化合物，此外还涉及包含这些化合物的制药组合物和套装。
• N-HETEROARYL COMPOUNDS WITH CYCLIC BRIDGING UNIT FOR THE TREATMENT OF PARASITIC DISEASES
  申请人：Berger Michael

  公开号：US20130203768A1

  公开（公告）日：2013-08-08

  This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.

  本发明涉及某些N-杂环芳基化合物，通常作为药物使用，更具体地作为动物药物。该药物可优选用于治疗蠕虫感染和寄生虫病的治疗，例如由蠕虫感染引起的寄生虫病。本发明还涉及使用该化合物制备药物和治疗方法，包括将该化合物用于需要治疗的动物的管理。本发明还涉及N-杂环芳基化合物的制备。此外，本发明还涉及包含该化合物的制药组合物和套装。
• Preparation and structural feature of (η3-Allyl)dicarbonylnitrosyliron complexes with planar chirality
  作者：Saburo Nakanishi、Hiroshi Yamaguchi、Kenji Okamoto、Toshikazu Takata

  DOI：10.1016/0957-4166(96)00276-5

  日期：1996.8

  The preparation of novel (eta(3)-Allyl)Fe(CO)(2)(NO) complexes with planar chirality has been achieved via separation of the diastereomeric complexes having chiral amide and ester groups as auxiliaries. X-ray analysis and CD spectra revealed the structural assignment of the complexes thus obtained. Copyright (C) 1996 Elsevier Science Ltd
• Synthesis and Structure−Activity Relationships of 6,7-Disubstituted 4-Anilinoquinoline-3-carbonitriles. The Design of an Orally Active, Irreversible Inhibitor of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor (EGFR) and the Human Epidermal Growth Factor Receptor-2 (HER-2)
  作者：Allan Wissner、Elsebe Overbeek、Marvin F. Reich、M. Brawner Floyd、Bernard D. Johnson、Nellie Mamuya、Edward C. Rosfjord、Carolyn Discafani、Rachel Davis、Xiaoqing Shi、Sridhar K. Rabindran、Brian C. Gruber、Fei Ye、William A. Hallett、Ramaswamy Nilakantan、Ru Shen、Yu-Fen Wang、Lee M. Greenberger、Hwei-Ru Tsou

  DOI：10.1021/jm020241c

  日期：2003.1.1

  A series of of 6,7-disubstituted-4-anilinoquinoline-3-carbonitrile derivatives that function as irreversible inhibitors of EGFR and HER-2 kinases have been prepared. These inhibitors have, at the 6-position, butynamide, crotonamide, and methacrylamide Michael acceptors bearing water-solublilizing substituents. These compounds were prepared by acylation of 6-amino-4-(arylamino)quinoline-3-carbonitriles with unsaturated acid chlorides or mixed anhydrides. We performed competitive reactivity studies showing that attaching a dialkylamino group onto the end of the Michael acceptor results in compounds with greater reactivity due to intramolecular catalysis of the Michael addition. This, along with improved water-solubility results in compounds with enhanced biological properties. We present molecular modeling results consistent with the proposed mechanism of inhibition. One compound, 5 (EKB-569), which shows excellent oral in vivo activity, was selected for further studies and is currently in phase I clinical trials for the treatment of cancer.