N~1~,N~1~-Dimethylethane-1,1-diamine | 116042-60-5

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: N~1~,N~1~-Dimethylethane-1,1-diamine
• 英文别名: 1-N',1-N'-dimethylethane-1,1-diamine
• CAS: 116042-60-5
• 化学式: C₄H₁₂N₂
• 分子量: 88.15
• InChiKey: MBBDOMNWCQRJJL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  6
• 可旋转键数：
  1
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-(5-amino-2-chloro-4-fluorophenyl)-7-chloro-1-ethyl-1,6-naphthyridin-2(1H)-one 、 N~1~,N~1~-Dimethylethane-1,1-diamine 、 N,N-二甲基甲酰胺 在 乙酸乙酯 、 Brine 、 magnesium sulfate 、 异丙醇 作用下， 以 水 为溶剂， 反应 36.0h， 以to provide 3-(5-amino-2-chloro-4-fluorophenyl)-7-(2-(dimethylamino)ethylamino)-1-ethyl-1,6-naphthyridin-2(1H)-one (0.98 g, 85% yield) as a white solid的产率得到3-(5-amino-2-chloro-4-fluorophenyl)-7-(2-(dimethylamino)ethylamino)-1-ethyl-1,6-naphthyridin-2(1H)-one
  参考文献：
  名称：

  Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases

  摘要：

  该发明涉及二氢萘啶和相关化合物；包含有效量二氢萘啶或相关化合物的组合物；以及治疗或预防增生性疾病的方法，包括给予有效量的二氢萘啶或相关化合物。

  公开号：

  US08461179B1

文献信息

• Certain heterocyclic thiazole derivatives and their therapeutic use
  申请人：Sanofi

  公开号：US05470855A1

  公开（公告）日：1995-11-28

  The invention relates to compounds of formula: ##STR1## in which: A is selected from O or S; B is selected from C or N; Z.sub.1 is selected from C.sub.1 -C.sub.4 alkylene or phenylene; Z.sub.2 is C.sub.1 -C.sub.4 alkylene; W is NR.sub.1 R.sub.2, in which R.sub.1 is selected from H or C.sub.1 -C.sub.4 alkyl and R.sub.2 is selected from H, C.sub.1 -C.sub.4 alkyl, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2 in which Q.sub.1 and Q.sub.2 are independently selected from H or C.sub.1 -C.sub.4 alkyl, SO.sub.2 Q.sub.3 or COQ.sub.3 in which Q.sub.3 is C.sub.1 -C.sub.4 alkyl, COOQ.sub.4 in which Q.sub.4 is selected from C.sub.1 -C.sub.4 alkyl or benzyl, or R.sub.1 and R.sub.2 taken together with N form a saturated heterocycle, or W is selected from C.sub.1 -C.sub.4 alkoxy or thioalkoxy, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2, pyridyl, imidazolyl or COOQ.sub.5 in which Q.sub.5 is C.sub.1 -C.sub.5 alkyl; R.sub.3 is not present when B is N, or is H, C.sub.1 -C.sub.8 alkyl or halogen; Ar.sub.1 is selected from optionally substituted phenyl, thienyl, furyl, indolyl, naphthyl or benzyl or Ar.sub.1 and R.sub.3 taken together form a phenylalkylene group; Ar.sub.2 is selected from pyrimidinyl, quinolyl, isoquinolyl, indolyl, isoindolyl or pyridyl, optionally substituted; as well as their salts. Use as medicines.

  本发明涉及以下式的化合物：##STR1##其中：A选择O或S; B选择C或N; Z.sub.1选择C.sub.1-C.sub.4烷基或苯基; Z.sub.2选择C.sub.1-C.sub.4烷基; W为NR.sub.1R.sub.2，其中R.sub.1选择H或C.sub.1-C.sub.4烷基，R.sub.2选择H、C.sub.1-C.sub.4烷基、CONQ.sub.1Q.sub.2或CSNQ.sub.1Q.sub.2，其中Q.sub.1和Q.sub.2独立选择H或C.sub.1-C.sub.4烷基、SO.sub.2Q.sub.3或COQ.sub.3，其中Q.sub.3选择C.sub.1-C.sub.4烷基、COOQ.sub.4，其中Q.sub.4选择C.sub.1-C.sub.4烷基或苄基，或R.sub.1和R.sub.2与N结合形成饱和的杂环，或W选择C.sub.1-C.sub.4烷氧基或硫基烷氧基、CONQ.sub.1Q.sub.2或CSNQ.sub.1Q.sub.2、吡啶基、咪唑基或COOQ.sub.5，其中Q.sub.5选择C.sub.1-C.sub.5烷基; 当B为N时，R.sub.3不存在，或为H、C.sub.1-C.sub.8烷基或卤素; Ar.sub.1选择可选取代的苯基、噻吩基、呋喃基、吲哚基、萘基或苄基，或Ar.sub.1和R.sub.3结合形成苯基烷基基团; Ar.sub.2选择嘧啶基、喹啉基、异喹啉基、吲哚基、异吲哚基或吡啶基，可选取代; 以及它们的盐。用作药物。
• Heterocyclic derivatives, process for their preparation and their
  申请人：Sanofi

  公开号：US05780468A1

  公开（公告）日：1998-07-14

  The invention relates to compounds of formula: ##STR1## in which: A is selected from O or S; B is selected from C or N; Z.sub.1 is selected from C.sub.1 -C.sub.4 alkylene or phenylene; Z.sub.2 is C.sub.1 -C.sub.4 alkylene; W is NR.sub.1 R.sub.2, in which R.sub.1 is selected from H or C.sub.1 -C.sub.4 alkyl and R.sub.2 is selected from H, C.sub.1 -C.sub.4 alkyl, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2 in which Q.sub.1 and Q.sub.2 are independently selected from H or C.sub.1 -C.sub.4 alkyl, SO.sub.2 Q.sub.3 or COQ.sub.3 in which Q.sub.3 is C.sub.1 -C.sub.4 alkyl, COOQ.sub.4 in which Q.sub.4 is selected from C.sub.1 -C.sub.4 alkyl or benzyl, or R.sub.1 and R.sub.2 taken together with N form a saturated heterocycle, or W is selected from C.sub.1 -C.sub.4 alkoxy or thioalkoxy, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2, pyridyl, imidazolyl or COOQ.sub.5 in which Q.sub.5 is C.sub.1 -C.sub.5 alkyl; R.sub.3 is not present when B is N, or is H, C.sub.1 -C.sub.8 alkyl or halogen; Ar.sub.1 is selected from optionally substituted phenyl, thienyl, furyl, indolyl, naphthyl or benzyl or Ar.sub.1 and R.sub.3 taken together form a phenylalkylene group; Ar.sub.2 is selected from pyrimidinyl, quinolyl, isoquinolyl, indolyl, isoindolyl or pyridyl, optionally substituted; as well as their salts. Use as medicines.

  本发明涉及式子的化合物：##STR1## 其中：A选自O或S; B选自C或N; Z.sub.1选自C.sub.1-C.sub.4烷基或苯基; Z.sub.2选自C.sub.1-C.sub.4烷基; W为NR.sub.1R.sub.2，其中R.sub.1选自H或C.sub.1-C.sub.4烷基，R.sub.2选自H，C.sub.1-C.sub.4烷基，CONQ.sub.1Q.sub.2或CSNQ.sub.1Q.sub.2，其中Q.sub.1和Q.sub.2独立选自H或C.sub.1-C.sub.4烷基，SO.sub.2Q.sub.3或COQ.sub.3，其中Q.sub.3为C.sub.1-C.sub.4烷基，COOQ.sub.4，其中Q.sub.4选自C.sub.1-C.sub.4烷基或苄基，或R.sub.1和R.sub.2与N结合形成饱和杂环，或W选自C.sub.1-C.sub.4烷氧基或硫代烷氧基，CONQ.sub.1Q.sub.2或CSNQ.sub.1Q.sub.2，吡啶基，咪唑基或COOQ.sub.5，其中Q.sub.5选自C.sub.1-C.sub.5烷基; 当B为N时，R.sub.3不存在，否则为H，C.sub.1-C.sub.8烷基或卤素; Ar.sub.1选自可选取代的苯基，噻吩基，呋喃基，吲哚基，萘基或苄基，或Ar.sub.1和R.sub.3结合形成苯基烷基基团; Ar.sub.2选自嘧啶基，喹啉基，异喹啉基，吲哚基，异吲哚基或吡啶基，可选取代; 以及它们的盐。用作药物。
• Heterocyclic derivatives process for their preparation and their
  申请人：Sanofi

  公开号：US05891894A1

  公开（公告）日：1999-04-06

  The invention relates to compounds of formula: ##STR1## in which: A is selected from 0 or S; B is selected from C or N; Z.sub.1 is selected from C.sub.1 -C.sub.4 alkylene or phenylene; Z.sub.2 is C.sub.1 -C.sub.4 alkylene; W is NR.sub.1 R.sub.2, in which R.sub.1 is selected from H or C.sub.1 -C.sub.4 alkyl and R.sub.2 is selected from H, C.sub.1 -C.sub.4 alkyl, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2 in which Q.sub.1 and Q.sub.2 are independently selected from H or C.sub.1 -C.sub.4 alkyl, SO.sub.2 Q.sub.3 or COQ.sub.3 in which Q.sub.3 is C.sub.1 -C.sub.4 alkyl, COOQ.sub.4 in which Q.sub.4 is selected from C.sub.1 -C.sub.4 alkyl or benzyl, or R.sub.1 and R.sub.2 taken together with N form a saturated heterocycle, or W is selected from C.sub.1 -C.sub.4 alkoxy or thioalkoxy, CONQ.sub.1 Q.sub.2 or CSNQ.sub.1 Q.sub.2, pyridyl, imidazolyl or COOQ.sub.5 in which Q.sub.5 is C.sub.1 -C.sub.5 alkyl; R.sub.3 is not present when B is N, or is H, C.sub.1 -C.sub.8 alkyl or halogen; Ar.sub.1 is selected from optionally substituted phenyl, thienyl, furyl, indolyl, naphthyl or benzyl or Ar.sub.1 and R.sub.3 taken together form a phenylalkylene group; Ar.sub.2 is selected from pyrimidinyl, quinolyl, isoquinolyl, indolyl, isoindolyl or pyridyl, optionally substituted; as well as their salts.

  本发明涉及以下式的化合物：##STR1## 其中：A选择为0或S；B选择为C或N；Z.sub.1选择为C.sub.1-C.sub.4烷基或苯基；Z.sub.2选择为C.sub.1-C.sub.4烷基；W为NR.sub.1R.sub.2，其中R.sub.1选择为H或C.sub.1-C.sub.4烷基，R.sub.2选择为H、C.sub.1-C.sub.4烷基、CONQ.sub.1Q.sub.2或CSNQ.sub.1Q.sub.2，其中Q.sub.1和Q.sub.2独立选择为H或C.sub.1-C.sub.4烷基、SO.sub.2Q.sub.3或COQ.sub.3，其中Q.sub.3为C.sub.1-C.sub.4烷基、COOQ.sub.4，其中Q.sub.4选择为C.sub.1-C.sub.4烷基或苄基，或R.sub.1和R.sub.2与N一起形成饱和杂环，或W选择为C.sub.1-C.sub.4烷氧基或硫代烷氧基、CONQ.sub.1Q.sub.2或CSNQ.sub.1Q.sub.2、吡啶基、咪唑基或COOQ.sub.5，其中Q.sub.5选择为C.sub.1-C.sub.5烷基；当B为N时，R.sub.3不存在，或为H、C.sub.1-C.sub.8烷基或卤素；Ar.sub.1选择为可选择取代的苯基、噻吩基、呋喃基、吲哚基、萘基或苄基，或Ar.sub.1和R.sub.3一起形成苯基烷基基团；Ar.sub.2选择为嘧啶基、喹啉基、异喹啉基、吲哚基、异吲哚基或吡啶基，可选择取代；以及它们的盐。
• DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES
  申请人：Deciphera Pharmaceuticals, Inc.

  公开号：US20140088075A1

  公开（公告）日：2014-03-27

  The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.

  本发明涉及二氢萘啉和相关化合物；包含有效量二氢萘啉或相关化合物的组合物；以及治疗或预防增殖性疾病的方法，其中包括给予有效量的二氢萘啉或相关化合物。
• Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
  申请人：Flynn Daniel L.

  公开号：US08461179B1

  公开（公告）日：2013-06-11

  The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.

  该发明涉及二氢萘啶和相关化合物；包含有效量二氢萘啶或相关化合物的组合物；以及治疗或预防增生性疾病的方法，包括给予有效量的二氢萘啶或相关化合物。