7-氯喹啉-2-胺 | 43200-95-9

• 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: 7-氯喹啉-2-胺
• 英文名称: 2-amino-7-chloroquinoline
• 英文别名: 2-Amino-7-chloroquinolin；Amino-2-chlor-7-chinolin；2-Amino-7-chloroquinolein；7-Chloroquinolin-2-amine
• CAS: 43200-95-9
• 化学式: C₉H₇ClN₂
• mdl: MFCD11877922
• 分子量: 178.621
• InChiKey: CVUUCFIVYYDLHL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933499090
• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

反应信息

• 作为反应物：
  描述：

  7-氯喹啉-2-胺 在 sodium hydroxide 作用下， 以 乙醇 、 水 为溶剂， 反应 3.5h， 生成 7-Chlorimidazo<1,2-a>chinolin-2-carbonsaeure
  参考文献：
  名称：

  Synthesis and oral antiallergic activity of carboxylic acids derived from imidazo[2,1-c][1,4]benzoxazines, imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles

  摘要：

  4H-Imidazo[2,1-c][1,4]benzoxazine-2-carboxylic acid (3) was found to possess potent activity in the IgE-induced rat passive cutaneous anaphylaxis model which may be predictive of clinical antiallergic activity. Compared to disodium cromoglycate (DSCG, 1), 3 was less active following iv administration but unlike DSCG showed very significant oral activity. To explore the structural requirements for this activity, a range of tricyclic compounds was prepared and their activities were measured. Individual 2-carboxylic acids derived from imidazo[1,2-a]quinolines, imidazo[1,2-a]quinoxalines, imidazo[1,2-a]quinoxalinones, pyrrolo[1,2-a]quinoxalinones, pyrrolo[2,3-a]quinoxalinones, and imidazo[2,1-b]benzothiazoles showed iv activities up to 10(3) times as potent as DSCG and many of them showed significant oral activity. From these, imidazo[1,2-a]quinoxaline-2-carboxylic acid 114 has been chosen for further development.

  DOI：

  10.1021/jm00401a009
• 作为产物：
  描述：

  2,7-二氯喹啉 在 氨 作用下， 生成 7-氯喹啉-2-胺
  参考文献：
  名称：

  1,4-Dithiino(2,3-c)pyrrole derivatives

  摘要：

  新化合物的公式为：##SPC1## 其中A是苯基、吡啶基、吡嗪啉基、2-、3-或4-喹啉基或萘啉基基团，或者是一个被卤素、烷基、烷氧基、氰基和硝基中的一个或两个原子或基团取代的该基团，R是烷基、烯基或羟基烷基，n为0或1，具有药理学特性，特别是作为镇静剂、抗惊厥剂、解痉剂和催眠剂的活性。

  公开号：

  US03948917A1

文献信息

• N-(1,8-naphthyridin-2-yl) amides and their pharmaceutical use
  申请人：Rhone-Poulenc Sante

  公开号：US04642308A1

  公开（公告）日：1987-02-10

  The invention provides novel substituted amides of formula: R--CONH--Het in which R is cycloalkyl, cyclohexadienyl, phenyl optionally substituted with one or 2 fluorine atoms or with a hydroxy radical, or substituted at position 3- or 4- with an alkyl or alkyloxy radical, or with a methylenedioxy radical at positions 3- and 4-, or at position 2- or 3- with a dialkylamino radical, or is 3-pyridyl, alkyloxy-3-pyridyl, thienyl, alkylthienyl, furyl, tetrahydropyridyl, pyridazinyl and alkylpyridazinyl, and Het is 2-quinolyl or 1,8-naphthyridin-2-yl, both optionally substituted at position 7- with a halogen atom or a hydroxymethyl, alkyl, alkyloxy, alkyloxyalkyloxy, alkenyloxy or alkynyloxy radical (of 3 or 4 carbon atoms), an alkylthio or benzylthio radical, a phenoxy radical which is optionally substituted (with fluorine, with chlorine or bromine at position 2-, or with an alkyloxy radical or 1 or 2 alkyl radicals) or with pyridyloxy or alkylpiperidyloxy, provided that, when Het is 2-quinolyl, R is other than phenyl, and that the radicals and alkyl portions contain 1 to 4 carbon atoms each in a linear or branched chain. The new products are useful as anxiolytics, hypnotics, anticonvulsants, antiepileptics and muscle relaxants. The invention also provides a process for the preparation of, and pharmaceutical compositions containing, the new compounds.

  该发明提供了一种新型的取代酰胺，化学式为：R--CONH--Het，其中R是环烷基、环己二烯基、苯基（可选择性地取代有一个或两个氟原子或一个羟基基团），或在3-或4-位置取代有烷基或烷氧基基团，或在3-和4-位置取代有亚甲二氧基基团，或在2-或3-位置取代有二烷基氨基基团，或是3-吡啶基、烷氧基-3-吡啶基、噻吩基、烷基噻吩基、呋喃基、四氢吡啶基、吡啶嗪基和烷基吡啶嗪基，Het是2-喹啉基或1,8-萘啉-2-基，两者可选择性地在7-位置取代有卤原子或羟甲基、烷基、烷氧基、烷氧基烷氧基、烯基氧基或炔基氧基基团（含有3或4个碳原子），烷硫基或苄硫基基团，苯氧基基团可选择性地取代（取代有氟、氯或溴在2-位置，或取代有烷氧基或1或2个烷基基团）或取代有吡啶氧基或烷基哌啶氧基，前提是当Het是2-喹啉基时，R不是苯基，且基团和烷基部分每个都含有1到4个碳原子，可以是线性或支链。这些新产品可用作抗焦虑药、催眠药、抗抽搐药、抗癫痫药和肌肉松弛剂。该发明还提供了一种制备这些新化合物的方法和含有这些新化合物的药物组合物。
• Substituted triazinyl amide derivatives and methods of use
  申请人：——

  公开号：US20030087908A1

  公开（公告）日：2003-05-08

  The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer and angiogenesis-related disease.

  本发明包括化合物、类似物、前药及其药物可接受的盐，药物组合物，以及用于预防与治疗癌症和与血管生成相关疾病的用途和方法。
• [EN] SUBSTITUTED ARYL-AMINE DERIVATIVES AND METHODS OF USE<br/>[FR] DÉRIVÉS AMINÉS À SUBSTITUTION ARYLE ET PROCÉDÉS D'UTILISATION
  申请人：AMGEN INC

  公开号：WO2006012374A1

  公开（公告）日：2006-02-02

  The present invention provides classes of compounds, including-their pharmaceutically acceptable derivatives, useful for treating angiogenesis and related diseases such as cancer. Formula I and II wherein R is a 9- or 10-membered heterocyclyl ring selected from 7-isoquinolinyl,..2-methyl-3-oxo-2,3-dihydroindazol-6-yl, [1,6]-naphthydrin-3-yl, [1,7]-naphthydrin-2-yl, 1-oxo-2,3-dihydrobenzofuran-4-yl, 3-oxo-2,3-dihydrobenzofuran-5-yl, dihydro-benzodioxinyl, 6-quinazolinyl, 2-amino-6-quinazolinyl, 4-methylamino-6-quinazolinyl, 2,4-diamino-6 quinazolinyl, 3-oxo-3,4-dihydro-1,4-benzoxazin-6-yl, 2,2-difluoro-l;3-benzodioxol-5-yl and 2,2,3,3 tetrafluoro-2,3-dihydro-l,4-benzodioxin-6-yl, each of which is optionally substituted with one or more substituents selected from halo, haloakyl, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, N-dimethylamino-C1-6-alkyl, N-dimethylamino-C1-6-alkoxy, amino, alkyl-carbonylamino, morpholino-sulfonyl, amino-sulfonyl, oxazolyl, pyrrolyl,4 morpholinyl, carboxyl, cyano, and acetyl; wherein R1 in formula I is selected from unsubstituted or substituted phenyl, 5-6 membered heteroaryl, 9-10 membered bicyclic heterocyclyl and 11-14 membered tricyclic heterocyclyl, and R1 in formula II is selected from specific bicyclic heterocycles.

  本发明提供了一类化合物，包括其药用可接受的衍生物，用于治疗血管生成和相关疾病，如癌症。其中R为从7-异喹啉基、2-甲基-3-氧代-2,3-二氢吲哚-6-基、[1,6]-萘啶-3-基、[1,7]-萘啶-2-基、1-氧代-2,3-二氢苯并呋喃-4-基、3-氧代-2,3-二氢苯并呋喃-5-基、二氢苯并二氧杂环基、6-喹唑啉基、2-氨基-6-喹唑啉基、4-甲氨基-6-喹唑啉基、2,4-二氨基-6-喹唑啉基、3-氧代-3,4-二氢-1,4-苯并噁嗪-6-基、2,2-二氟-1,3-苯并二氧杂环-5-基和2,2,3,3-四氟-2,3-二氢-1,4-苯并二氧杂环-6-基中选择的9-或10-成员杂环基，其中每个基可选择地被一个或多个来自卤素、卤代烷基、C1-6烷基、C2-8烯基、C2-8炔基、N-二甲氨基-C1-6-烷基、N-二甲氨基-C1-6-烷氧基、氨基、烷基-羰基氨基、吗啉磺酰基、氨基磺酰基、噁唑基、吡咯基、吗啉基、羧基、氰基和乙酰基的取代基取代；其中式I中的R1从未取代或取代的苯基、5-6成员杂芳基、9-10成员双环杂环基和11-14成员三环杂环基中选择，式II中的R1从特定的双环杂环基中选择。
• Substituted alkylamine derivatives and methods of use
  申请人：Amgen Inc.

  公开号：US20030225106A1

  公开（公告）日：2003-12-04

  Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选定的胺对预防治疗疾病有效，如血管生成介导的疾病。本发明包括新的化合物、类似物、前药和药用可接受的盐，药物组合物和预防治疗疾病和其他疾病或状况的方法，包括癌症等。本发明还涉及制造这类化合物的过程以及在此类过程中有用的中间体。
• Substituted amine derivatives and methods of use
  申请人：Amgen Inc.

  公开号：US20030203922A1

  公开（公告）日：2003-10-30

  Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

  选定的胺类化合物对于预防和治疗疾病，如血管生成介导的疾病，具有有效性。该发明涵盖了新颖的化合物、类似物、前药和其药用可接受盐，用于预防和治疗涉及癌症等疾病和其他疾患或病况的药物组合物和方法。该发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。