吡啶并[2,3,4-kl]吖啶 | 144630-86-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 吡啶并[2,3,4-kl]吖啶
• 英文名称: pyrido<2,3,4-kl>acridine
• 英文别名: 7H-pyrido[2,3,4-kl]acridine；Pyrido[2,3,4 kl]acridin；8,14-diazatetracyclo[7.7.1.02,7.013,17]heptadeca-1(17),2,4,6,9,11,13,15-octaene
• CAS: 144630-86-4
• 化学式: C₁₅H₁₀N₂
• 分子量: 218.258
• InChiKey: FIMAREBXEDRAIE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  17
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  24.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  吡啶并[2,3,4-kl]吖啶 在 tris-(dibenzylideneacetone)dipalladium(0) 、 正丁基锂 、 三叔丁基膦 、 sodium t-butanolate 作用下， 以 四氢呋喃 、 甲苯 为溶剂， 反应 36.0h， 生成 spiro[benzo[b]quinolino[4,3,2,1-lmn][1,7]phenanthroline-10,9'-fluorene]
  参考文献：
  名称：

  KR2023/109821

  摘要：

  公开号：
• 作为产物：
  描述：

  4-氯喹啉 在 四(三苯基膦)钯 盐酸 、 硫酸 、 sodium carbonate 、 sodium nitrite 作用下， 以 乙二醇二甲醚 、 乙醇 、 水 、 邻二氯苯 为溶剂， 反应 49.5h， 生成 吡啶并[2,3,4-kl]吖啶
  参考文献：
  名称：

  Synthesis of the benzo-β-carboline isoneocryptolepine: the missing indoloquinoline isomer in the alkaloid series cryptolepine, neocryptolepine and isocryptolepine

  摘要：

  7H-Indolo[2,3-c]quinoline has been synthesized in two steps via a new approach starting from commercially available 3-bromoquinoline and 2-bromoaniline. The new methodology consists of two consecutive palladium-catalyzed reactions: a selective Buchwald/Hartwig amination followed by an intramolecular Heck-type reaction. Alternatively, the same skeleton has also been prepared via the combination of a Suzuki arylation with an intramolecular nitrene insertion starting front 4-chloroquinotine and [2-[(2-2dimethylpropanoyl)amino]phenyl}boronic acid. Selective methylation of 7H-indolo[2.3-c]quinotine yielded 5-methyl-5H-indolo[2,3c]quinoline (Isoneocryptolepine) which is an interesting new lead compound in the search for new antiplasmodial drugs. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2004.11.073

文献信息

• Antitumour 1,5-diazaanthraquinones
  申请人：——

  公开号：US20020099066A1

  公开（公告）日：2002-07-25

  1 Compounds having formula (I) wherein R 3 , R 4 , R 7 , and R 8 are independently selected from the group consisting of hydrogen, lower alkyl, halogen, amine, mono(lower)alkylamine, di(lower)alkylamine, phenyl, or substituted phenyl possess antitumor activity and are new with the exception of the compound in which R 3 , R 4 , R 7 , R 8 are all hydrogen and the compound in which R 3 and R 7 are hydrogen, R 4 chlorine, and R 8 is a 2-nitrophenyl group.

  具有公式(I)的化合物，其中R3、R4、R7和R8独立地选自包括氢、低级烷基、卤素、胺、单（低级）烷基胺、二（低级）烷基胺、苯基或取代苯基的组，具有抗肿瘤活性，除了R3、R4、R7、R8均为氢的化合物和R3和R7为氢，R4为氯，R8为2-硝基苯基的化合物外，都是新的。
• Cytotoxic compounds: derivatives of the pyrido [2,3,4-kl]acridine ring system
  申请人：Universidad Complutense de madrid

  公开号：US20020128281A1

  公开（公告）日：2002-09-12

  Compounds of formula (I), wherein X is selected from the group consisting of O, and NR 3 , where R 3 represents a lower alkyl group; Y is selected from the group consisting of CH and N; R 1 and R 2 are independently selected from the group consisting of NH 2 , NHR 4 and NR 5 2 , where R 4 and R 5 each represent a lower alkyl group, or R 1 and R 2 together represent a cycle selected from (a), (b) and (c), wherein R 6 , R 7 and R 8 are independently selected from the group consisting of hydrogen atoms, lower alkyl groups, hydroxy groups and lower alkoxy groups; and Z is selected from the group consisting of O.

  式（I）的化合物，其中X从O和NR3组成的组中选择，其中R3代表较低的烷基基团；Y从CH和N组成的组中选择；R1和R2分别从NH2、NHR4和NR52组成的组中独立选择，其中R4和R5各自代表较低的烷基基团，或者R1和R2一起代表从(a)、(b)和(c)中选择的环，其中R6、R7和R8从氢原子、较低的烷基基团、羟基和较低的烷氧基组成的组中独立选择；Z从O组成的组中选择。
• N8, n13 -disubstituted quino[4,3,2-kl]acridinium salts as therapeutic agents
  申请人：——

  公开号：US20040063739A1

  公开（公告）日：2004-04-01

  The present invention pertains to certain N 8 ,N 13 -disubstituted quino[4,3,2-kl]acridinium salts of formula (Q − ) which inhibit telomerase wherein: p is an integer from 0 to 4; q is an integer from 0 to 3; r is an integer from 0 to 4; each R A is —H or a ring substituent; each R B is —H or a ring substituent; each R C is —H or a ring substituent; R N8 is a nitrogen substituent; R N13 is a nitrogen substituent; and, Q is an anion. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.

  本发明涉及某些N8，N13-二取代喹诺[4,3,2-kl]吖啶盐的化合物，其化学式为(Q−)，用于抑制端粒酶，其中：p为0至4的整数；q为0至3的整数；r为0至4的整数；每个RA为—H或环取代基；每个RB为—H或环取代基；每个RC为—H或环取代基；RN8为氮取代基；RN13为氮取代基；Q为阴离子。本发明还涉及包括这些化合物的药物组合物，以及在体外和体内使用这些化合物和组合物来抑制端粒酶，调节细胞增殖，并用于治疗增殖性疾病，如癌症。
• Synthesis of pyrido[2,3,4-kl]acridines a building block for the synthesis of pyridoacridine alkaloids
  作者：Gari Gellerman、Amira Rudi、Yoel Kashman

  DOI：10.1016/s0040-4039(00)61150-4

  日期：1992.9

  Two new syntheses have been developed for the preparation of substituted pyrido[2,3,4-kl]acridines. The first synthesis involves a Skraup reaction and a nitrene insertion whereas the second includes a new pyridine ring synthesis starting from a 1-amino group on acridine and taking advantage of the active 9-position of the latter heterocycle.

  已经开发出两种新的合成方法用于制备取代的吡啶并[2,3,4-kl] ac啶。第一种合成涉及Skraup反应和氮烯插入，而第二种合成包括新的吡啶环合成，该合成是从ring啶上的1-氨基开始并利用后者杂环的活性9位进行的。
• Potassium channel mediated delivery of agents through the blood-brain barrier
  申请人：Black L. Keith

  公开号：US20050089473A1

  公开（公告）日：2005-04-28

  This invention includes pharmaceutical compositions, methods and kits for the treatment or diagnosis of a malignant tumors, including brain tumors, and diseases or disorders characterized by abnormal brain tissue.

  本发明包括用于治疗或诊断恶性肿瘤（包括脑肿瘤）以及以脑组织异常为特征的疾病或紊乱的药物组合物、方法和试剂盒。