2,3-dichloroaniline hydrochloride

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2,3-dichloroaniline hydrochloride
• 英文别名: 2,3-dichlorobenzenamine monohydrochloride；2,3-dichloroaniline;hydron;chloride
• 化学式: C₆H₅Cl₂N*ClH
• 分子量: 198.479
• InChiKey: RAEZMDXXPWDHRQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.0
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  26
• 氢给体数：
  2
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2,3-dichloroaniline hydrochloride 在 sodium hydroxide 作用下， 生成 (2,3-dichloro-phenylhydrazono)-malonic acid
  参考文献：
  名称：

  552.一种新的cinnoline合成。第一部分。中草酰氯苯hydr的环化反应，生成取代的4-羟基cinnoline-3-羧酸

  摘要：

  DOI：

  10.1039/jr9610002828
• 作为产物：
  描述：

  N,N-dichloro-aniline 、 α-Chlor-α-methyl-β-(2,3-dichlor-phenyl)-propionaldehyd 在 盐酸 、 sodium nitrite 、 水 、 CaO 、 2-甲基丙烯醛 、 氯化亚铜 、 diazonium salt 作用下， 以 溶剂黄146 为溶剂， 120.0 ℃ 、177.32 Pa 条件下， 反应 12.5h， 生成 2,3-dichloroaniline hydrochloride
  参考文献：
  名称：

  Process for the arylation of olefines

  摘要：

  一种芳基化烯烃化合物的方法，通过将芳基基团加到所述烯烃化合物的双键上，包括在含有较低的烷酸的水溶性酸性溶液中重氮化芳胺，以形成一种芳基重氮盐溶液，并在有机溶剂中，在催化剂作用下的有效量的卤化铜的存在下，将所述芳基重氮盐溶液与烯烃化合物反应。烷酸的量为所用溶剂总量的约15％至37％体积。烷酸最好是乙酸，卤化铜最好是氯化亚铜。

  公开号：

  US04145362A1

文献信息

• 4-quinolinyl derivatives
  申请人：Janssen Pharmaceutica N.V.

  公开号：US05589484A1

  公开（公告）日：1996-12-31

  The present invention is concerned with novel quinoline derivatives having anti-Helicobacter activity of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, the stereochemically isomeric forms thereof, the quaternized forms thereof and the N-oxides thereof, wherein --A-- represents a bivalent radical of formula --N.dbd.CH--CH.dbd.CH-- (a), --CH.dbd.N--CH.dbd.CH-- (b), --N.dbd.N--CH.dbd.CH-- (c), --N.dbd.CH--N.dbd.CH-- (d), --N.dbd.CH--CH.dbd.N-- (e), --CH.dbd.N--N.dbd.CH-- (f), --N.dbd.N--N.dbd.CH-- (g), --N.dbd.N--CH.dbd.N-- (h), or --CH.dbd.CH--CH.dbd.CH-- (i); R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently represent hydrogen, halo, hydroxy, C.sub.1-4 alkyloxy, C.sub.1-4 alkyl, trifluoromethyl, amino, mono- or di(C.sub.1-4 alkyl)amino or nitro, provided that when one substituent on a phenyl group is a nitro then the other substituents on said phenyl group are other than nitro; novel compositions comprising said compounds, processes of preparing said compounds and compositions and methods for treating subjects suffering from disorders or afflictions associated with Helicobacter infection.

  本发明涉及具有抗幽门螺杆菌活性的新型喹啉衍生物，其化学式为##STR1## 其药用可接受的酸盐，其立体化学异构体形式，其季铵盐形式和其N-氧化物，其中-A-代表化学式--N.dbd.CH--CH.dbd.CH-- (a)，--CH.dbd.N--CH.dbd.CH-- (b)，--N.dbd.N--CH.dbd.CH-- (c)，--N.dbd.CH--N.dbd.CH-- (d)，--N.dbd.CH--CH.dbd.N-- (e)，--CH.dbd.N--N.dbd.CH-- (f)，--N.dbd.N--N.dbd.CH-- (g)，--N.dbd.N--CH.dbd.N-- (h)，或--CH.dbd.CH--CH.dbd.CH-- (i)的二价基团；R.sup.1、R.sup.2、R.sup.3、R.sup.4、R.sup.5、R.sup.6和R.sup.7分别独立地代表氢、卤素、羟基、C.sub.1-4烷氧基、C.sub.1-4烷基、三氟甲基、氨基、单烷基或双烷基氨基或硝基，但当苯基上的一个取代基是硝基时，那么所述苯基上的其他取代基除硝基外；包含所述化合物的新型组合物，制备所述化合物和组合物的方法以及治疗患有与幽门螺杆菌感染相关的疾病或痛苦的方法。
• Synthesis of Quinobenzo-1,4-thiazines from Diquino-1,4-dithiin and 2,2’-Dichloro-3,3’-diquinolinyl Disulfide
  作者：Krystian Pluta、Małgorzata Jeleń

  DOI：10.3987/com-09-11736

  日期：——

  10-substituted quinobenzo-1,4-thiazines (benzo[b]-1-azaphenothiazines) (5) and (10), has been worked out from diquino-1,4-dithiin (5,12-diaza-6,13-dithiapentacene) (2) as fusion reactions with aniline hydrochlorides (8)·HCl via the 1,4-dithiin ring opening and the 1,4-thiazine ring closure. The better results were obtained when 2,2'-dichloro-3,3'-diquinolinyl disulfide (9) reacted with anilines (8) in MEDG

  合成新型四环氮杂吩噻嗪，6-, 8-, 9- 和 10-取代的 quinobenzo-1,4-thiazines (benzo[b]-1-azaphenothiazines) (5) 和 (10), 从diquino-1,4-dithiin (5,12-diaza-6,13-​​dithiapentacene) (2) 通过 1,4-dithiin 开环和 1,4-thiazine 与盐酸苯胺 (8)·HCl 发生融合反应闭环。当 2,2'-二氯-3,3'-二喹啉基二硫化物 (9) 与苯胺 (8) 在 MEDG 中反应时，获得了更好的结果。选择的 6H-quinobenzo-1,4-thiazines (5a) (5c) 和 (5g) 通过使用烷基卤化物的 N-烷基化转化为 6-烷基衍生物 (10a-10n)。6-甲基衍生物（10a）的同核NOE实验证实产物结构为醌[3,2-b]苯并[1,4]噻嗪。
• Synthesis and Pharmacological Evaluation of <i>N</i>-(2,5-Disubstituted phenyl)-<i>N</i>‘-(3-substituted phenyl)-<i>N</i>‘-methylguanidines As <i>N</i>-Methyl-<scp>d</scp>-aspartate Receptor Ion-Channel Blockers
  作者：Lain-Yen Hu、Junqing Guo、Sharad S. Magar、James B. Fischer、Kathleen J. Burke-Howie、Graham J. Durant

  DOI：10.1021/jm970459c

  日期：1997.12.1

  In the mammalian central nervous system, the N-methyl-D-aspartate (NMDA) subclass of glutamate receptors may play an important role in brain diseases such as stroke, brain or spinal cord trauma, epilepsy, and certain neurodegenerative diseases. Compounds which specifically antagonize the actions of the neurotransmitter glutamate at the NMDA receptor ion-channel site offer a novel approach to treating these disorders. CERESTAT (4, aptiganel CNS 1102) is currently undergoing clinical trial for the treatment of traumatic brain injury and stroke. Previously, we reported that analogues of N-1-naphthyl-N'-(3-ethylphenyl)-N'-methylguanidine (4) bound to the NMDA receptor ion-channel site with high potency and selectivity. Recently, molecules active at both a receptors and NMDA receptor sites were investigated. A series of substituted diphenylguanidines 6 which are structurally related to N-1-naphthyl-N'-(3-ethylphenyl)-N'-methylguanidine was prepared. Compounds containing appropriate substitution pattern in one of the phenyl rings of diphenylguanidines displayed high affinity. For example, N-(2,5-dibromophenyl)-N'-(3-ethylphenyl)-N'-methylguanidine (27b, R-2 = R-5 = Br, R-3 = C2H5) exhibited potency at both a receptors and NMDA receptor sites; 27b also showed high efficacy in vivo in a neonatal rat excitotoxicity model. Further studies indicated that substituent effects were important in this compound series, and 2,5-disubstituted phenyl was the preferred substitution pattern for high-affinity binding at NMDA receptor sites. Bromo and methylthio were the optimal substituents for the R-2 and R-5 positions of the 2,5-disubstituted phenyl group, respectively. N-(2-Bromo-5-(methylthio)phenyl)-N'-(3-ethylphenyl)- N'-methylguanidine (34b, R-2 = Br, R-5 = SMe, R-3 = C2H5) was highly active at NMDA receptor sites. We found that the binding affinity of guanidines of type 6 could be further enhanced with the appropriate substitution at R-3. Optimal activity in this series are afforded by 43b and 44b (R-2 = Cl or Br, R-5 = R-3 = SCH3). Both 43b and 44b bound to NMDA receptor sites with high potency and selectivity (K-i vs [H-3]MK-801: 1.87 and 1.65 nM, respectively); these compounds are active in vivo in various animal models of neuroprotection. The structure-activity relationships for-these compounds at the NMDA receptor ion-channel site are discussed.
• Heesing,A.; Schmaldt,W., Chemische Berichte, 1978, vol. 111, p. 320 - 334
  作者：Heesing,A.、Schmaldt,W.

  DOI：——

  日期：——
• CH594614
  申请人：——

  公开号：——

  公开（公告）日：——