6-(furan-2-yl)pyridazin-3-amine | 38530-09-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 6-(furan-2-yl)pyridazin-3-amine
• 英文别名: 3-Amino-6-(2-furanyl)pyridazine
• CAS: 38530-09-5
• 化学式: C₈H₇N₃O
• 分子量: 161.163
• InChiKey: JWUIYTBBBRZUFC-UHFFFAOYSA-N

物化性质

• 沸点：
  381.7±27.0 °C(Predicted)
• 密度：
  1.276±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  64.9
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  6-(furan-2-yl)pyridazin-3-amine 、 4-溴丁酸乙酯 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 、 水 为溶剂， 反应 5.0h， 生成 3-aminopyridazine
  参考文献：
  名称：

  Competitive antagonism of insect GABA receptors by iminopyridazine derivatives of GABA

  摘要：

  A series of 4-(6-imino-3-aryl/heteroarylpyridazin-1-yl) butanoic acids were synthesized and examined for antagonism of GABA receptors from three insect species. When tested against small brown planthopper GABA receptors, the 3,4-methylenedioxyphenyl and the 2-naphthyl analogues showed complete inhibition of GABA-induced fluorescence changes at 100 mu M in assays using a membrane potential probe. Against common cutworm GABA receptors, these analogues displayed approximately 86% and complete inhibition of GABA-induced fluorescence changes at 100 mu M, respectively. The 4-biphenyl and 4-phenoxyphenyl analogues showed moderate inhibition at 10 mu M in these receptors, although the inhibition at 100 mu M was not complete. Against American cockroach GABA receptors, the 4-biphenyl analogue exhibited the greatest inhibition (approximately 92%) of GABA-induced currents, when tested at 500 mu M using a patch-clamp technique. The second most active analogue was the 2-naphthyl analogue with approximately 85% inhibition. The 3-thienyl analogue demonstrated competitive inhibition of cockroach GABA receptors. Homology modeling and ligand docking studies predicted that hydrophobic 3-substituents could interact with an accessory binding site at the orthosteric binding site. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2012.07.049
• 作为产物：
  描述：

  3-氨基-6-氯哒嗪 、 2-(三丁基锡烷基)呋喃 在 bis-triphenylphosphine-palladium(II) chloride 作用下， 以 四氢呋喃 为溶剂， 反应 20.0h， 以89%的产率得到6-(furan-2-yl)pyridazin-3-amine
  参考文献：
  名称：

  钯催化交叉偶联反应合成3-氨基-6-（杂）芳基哒嗪的新方法1

  摘要：

  经由钯的3-氨基-6-（杂）arylpyridazines合成上的3-氨基-6-氯哒嗪（催化的交叉偶联反应（铃木，的Stille）1A）和3-氨基-6- iodopyridazine（1B）进行了研究。结果比较表明，无需从1b开始。还描述了一种由1a合成化合物1b的改进方法。

  DOI：

  10.1016/s0040-4020(00)00083-1

文献信息

• LIGANDS FOR ANTIBODY AND FC-FUSION PROTEIN PURIFICATION BY AFFINITY CHROMOTOGRAPHY IV
  申请人：GRAFFINITY PHARMACEUTICALS GMBH

  公开号：US20160009760A1

  公开（公告）日：2016-01-14

  The present invention relates to the use, for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) L-(Sp) v -Ar 1 —Am—Ar 2 (I) wherein L, SP, Ar 1 , AM, Ar 2 and v are defined herein.

  本发明涉及使用含有配体取代基质来亲和纯化抗体或抗体片段，所述基质包括支持材料和至少一个与支持材料共价结合的配体，所述配体由式(I)所表示：L-(Sp)v-Ar1—Am—Ar2(I)，其中L、SP、Ar1、AM、Ar2和v在此处有定义。
• [EN] INHIBITORS OF ANOCTAMIN 6 PROTEIN AND USES THEREOF<br/>[FR] INHIBITEURS DE LA PROTÉINE ANOCTAMINE 6 ET LEURS UTILISATIONS
  申请人：ILDONG PHARMACEUTICAL CO LTD

  公开号：WO2022157686A1

  公开（公告）日：2022-07-28

  The present invention relates to a new compound that can inhibit an anoctamin 6 protein, a composition comprising the compound, a method for preparing the compound, and a method for using the compound or composition.

  本发明涉及一种新化合物，可以抑制anoctamin 6蛋白质，包括该化合物的组合物，制备该化合物的方法，以及使用该化合物或组合物的方法。
• Mild and Direct Access to 7-Substituted-4-trifluoromethylpyrimido[1,2-b]pyridazin-2-one Systems
  作者：Mohamed Abarbri、Julien Petrignet、Emilie Thiery、Laurence Silpa

  DOI：10.1055/s-0033-1340664

  日期：——

  New and efficient methods for the synthesis of 7-substituted-4-trifluoromethylpyrimido[1,2-b]pyridazin-2-one derivatives using either two-step Suzuki/heterocyclization, or two-step heterocyclization/substitution sequences are developed. A variety of substituted products are obtained in good to excellent yields from 3-amino-6-chloropyridazine and ethyl 4,4,4-trifluorobut-2-ynoate.
• US9745339B2
  申请人：——

  公开号：US9745339B2

  公开（公告）日：2017-08-29
• [EN] LIGANDS FOR ANTIBODY AND FC-FUSION PROTEIN PURIFICATION BY AFFINITY CHROMOTOGRAPHY IV<br/>[FR] LIGANDS POUR ANTICORPS ET PURIFICATION DE PROTÉINE DE FUSION À FRAGMENT CONSTANT PAR CHROMATOGRAPHIE D'AFFINITÉ IV
  申请人：GRAFFINITY PHARMACEUTICALS GMBH

  公开号：WO2013117707A1

  公开（公告）日：2013-08-15

  The present invention relates to the use, for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) L-(Sp)v-Ar1-Am-Ar2 wherein L is the linking point on the support material to which the ligand is attached; Sp is a spacer group; v is 0 or 1; Am is an amide group -NR1-C(O)-, and wherein either NR1 is attached to Ar1 and -C(O)- is attached to Ar2, or -C(O)- is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, more preferably hydrogen or methyl; and most preferably hydrogen; Ar1 is a 5-, 6- or 7-membered mononuclear aromatic ring or partially saturated aromatic ring connected to Sp or L via a chemical bond and which is optionally furthermore (a) attached to a further 5- or 6-membered mononuclear aromatic ring via a chemical bond; or (b) fused to a mononuclear or binuclear aromatic ring as part of a multinuclear ring system wherein Ar1 is directly connected to Am via a chemical bond present on the said 5-, 6- or 7- membered aromatic ring constituting Ar1, or indirectly via a chemical bond which is either present at the further 5- or 6-membered aromatic ring attached to Ar1, or on the further 5- or 6- membered aromatic ring fused to Ar1; and wherein Ar1 is either not further substituted or attached to at least one substituent selected from C1 to C4 alkyl; C3 and C4 cycloalkyl; C2 to C4 alkenyl;; C2 to C4 alkynyl; a halogen; C1 to C4 haloalkyl;;; hydroxyl-substituted C1 to C4 alkyl; C1 to C4 alkoxy; hydroxyl-substituted C1 to C4 alkoxy; halogen-substituted C1 to C4 alkoxy; C1 to C4 alkylamino; C1 to C4 alkylthio; -NO2; =O; =S; =NH; -OH?; and combinations thereof; Ar2 is a 5- or 6-membered mononuclear aromatic ring which is unsubstituted, or via a chemical bond attached to at least one substituent selected from C1 to C6 alkyl; C3 to C6 cycloalkyl; C2 to C6 alkenyl; C5 and C6 cycloalkenyl; C2 to C6 alkynyl; a halogen; C1 to C6 haloalkyl; hydroxyl-substituted C1 to C6 alkyl; C1 to C6 alkoxy; hydroxyl-substituted C1 to C6 alkoxy; halogen-substituted C1 to C6 alkoxy; C1 to C6 alkylamino; C1 to C6 alkylthio; carbamoyl; methylenedioxy; ethylenedioxy; -OH; SH; a 5- or 6-membered mononuclear aromatic ring; and combinations thereof; and wherein Ar2 optionally, further to the substituents to which it may be attached via a chemical bond as cited above, is fused to a 5- or 6-membered mononuclear aromatic ring as part of a multinuclear ring system.