2-氯-6,7-二氢-5H-环戊并[d]嘧啶 | 1030377-43-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 中文名称: 2-氯-6,7-二氢-5H-环戊并[d]嘧啶
• 英文名称: 2-chloro-6,7-dihydro-5H-cyclopenta[d]pyrimidine
• CAS: 1030377-43-5
• 化学式: C₇H₇ClN₂
• 分子量: 154.599
• InChiKey: YRPKTWHLIYZWGY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-氯-6,7-二氢-5H-环戊并[d]嘧啶 生成 2-{(5R)-5-methyl-4-[2-(2H-1,2,3-triazol-2-yl)benzoyl]-1,4-diazepan-1-yl}-6,7-dihydro-5H-cyclopenta[d]pyrimidine
  参考文献：
  名称：

  Substituted diazepan orexin receptor antagonists

  摘要：

  本发明涉及替代二氮杂环丙烷化合物，其为促进睡眠蛋白受体的拮抗剂，可用于治疗或预防神经和精神疾病，以及涉及促进睡眠蛋白受体的疾病。该发明还涉及包含这些化合物的药物组合物，以及利用这些化合物和组合物在预防或治疗涉及促进睡眠蛋白受体的疾病中的用途。

  公开号：

  US20080132490A1
• 作为产物：
  描述：

  2,4-二氯-5,6-三甲基嘧啶 生成 2-氯-6,7-二氢-5H-环戊并[d]嘧啶
  参考文献：
  名称：

  Substituted diazepan orexin receptor antagonists

  摘要：

  本发明涉及替代二氮杂环丙烷化合物，其为促进睡眠蛋白受体的拮抗剂，可用于治疗或预防神经和精神疾病，以及涉及促进睡眠蛋白受体的疾病。该发明还涉及包含这些化合物的药物组合物，以及利用这些化合物和组合物在预防或治疗涉及促进睡眠蛋白受体的疾病中的用途。

  公开号：

  US20080132490A1

文献信息

• [EN] THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS<br/>[FR] COMPOSÉS AMINOHÉTÉROARYLE À SUBSTITUTION THIAZOLE UTILISÉS COMME INHIBITEURS DE LA TYROSINE KINASE SPLÉNIQUE
  申请人：MERCK SHARP & DOHME

  公开号：WO2015095444A1

  公开（公告）日：2015-06-25

  The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).

  该发明提供了某些噻唑取代氨基杂环芳烃化合物的化学式(I) (I)，或其药用可接受的盐，其中环R1、R2、R3、R4、环A以及下标n1、n2和r如本文所定义。该发明还提供了包含这些化合物的药物组合物，以及利用这些化合物治疗由脾酪氨酸激酶（Syk）介导的疾病或症状的方法。
• 2-(Pyridin-2-yl)-pyrimidines and Their Use for Controlling Harmful Fungi
  申请人：Grammenos Wassilios

  公开号：US20100286175A1

  公开（公告）日：2010-11-11

  The invention relates to 2-(pyridin-2-yl)-pyrimidine compounds of general formula (I) and their use for controlling pathogenic fungi and as plant protection products that, as an active constituent, contain compounds of this type: In general formula (I), k represents 0, 1, 2, 3; m represents 0, 1, 2, 3, 4 or 5; n represents 1, 2, 3, 4 or 5; R 1 , independent of one another, represents halogen, OH, CN, NO 2 , C 1 -C 4 alkyl, C 1 -C 4 alkyl halide, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy halide, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 8 cycloalkyl, C 1 -C 4 alkoxy-C 1 -C 4 alkyl, amino, phenoxy, which is optionally substituted by halogen or C 1 -C 4 alkyl, NHR, NR 2 , C(R a )═N—OR b , S(═O) p A 1 or C(═O)A 2 , or two radicals R 1 bound to adjacent carbon atoms can, together, also represent a group —O-Alk-O—, wherein Alk represents a linear or branched C 1 -C 4 alkylene, and 1, 2, 3 or 4 hydrogen atoms can also be replaced by halogen; R 2 represents C 1 -C 4 alkyl halide, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy halide, hydroxy, halogen, CN or NO 2 ; whereby R 2 can also represent hydrogen or C 1 -C 4 alkyl when at least one of the three following conditions is fulfilled: n represents 3, 4 or 5; k represents 1, 2 or 3; if m is not equal to 0, at least one of the radicals R 1 represents a radical that differs from halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy and C 1 -C 4 alkyl halide, and; R 3 represents C 1 -C 4 alkyl.

  本发明涉及一般式（I）的2-(吡啶-2-基)-嘧啶化合物及其用于控制病原真菌和作为植物保护产品的用途，作为活性成分含有此类化合物：在一般式（I）中，k表示0、1、2或3；m表示0、1、2、3、4或5；n表示1、2、3、4或5；R1独立地表示卤素、OH、CN、NO2、C1-C4烷基、C1-C4烷基卤素、C1-C4烷氧基、C1-C4烷氧基卤素、C2-C4烯基、C2-C4炔基、C3-C8环烷基、C1-C4烷氧基-C1-C4烷基、氨基、苯氧基，该苯氧基可选择地被卤素或C1-C4烷基取代、NHR、NR2、C(Ra)═N—ORb、S(═O)pA1或C(═O)A2，或者相邻碳原子上结合的两个基R1也可以表示一个基团—O-Alk-O—，其中Alk表示直链或支链的C1-C4烷基，1、2、3或4个氢原子也可以被卤素取代；R2表示C1-C4烷基卤素、C1-C4烷氧基、C1-C4烷氧基卤素、羟基、卤素、CN或NO2；当满足以下至少三个条件之一时，R2也可以表示氢或C1-C4烷基：n表示3、4或5；k表示1、2或3；如果m不等于0，则至少一个基团R1表示与卤素、C1-C4烷基、C1-C4烷氧基和C1-C4烷基卤素不同的基团；R3表示C1-C4烷基。
• Substituted diazepan compounds as orexin receptor antagonists
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2392572A1

  公开（公告）日：2011-12-07

  The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

  本发明涉及取代的二氮杂环庚烷化合物，它们是奥曲肽受体的拮抗剂，可用于治疗或预防涉及奥曲肽受体的神经和精神紊乱及疾病。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在预防或治疗涉及奥曲肽受体的此类疾病中的用途。
• THIAZOLE-SUBSTITUTED AMINOHETEROARYLS AS SPLEEN TYROSINE KINASE INHIBITORS
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP3083560B1

  公开（公告）日：2021-10-27
• 2-(Pyridin-2-Yl)-Pyrimidines and Their Use for Controlling Harmful Fungi
  申请人：Grammenos Wassilios

  公开号：US20080027085A1

  公开（公告）日：2008-01-31

  The invention relates to 2-(pyridin-2-yl)-pyrimidine compounds of general formula (I) and their use for controlling pathogenic fungi and as plant protection products that, as an active constituent, contain compounds of this type, whereby: k represents 0, 1, 2, 3; m represents 0, 1, 2, 3, 4 or 5; n represents 1, 2, 3, 4 or 5; R 1 , independent of one another, represents halogen, OH, CN, NO 2 , C 1 -C 4 alkyl, C 1 -C 4 alkyl halide, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy halide, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, C 3 -C 8 cycloalkyl, C 1 -C 4 alkoxy-C 1 -C 4 alkyl, amino, phenoxy, which is optionally substituted by halogen or C 1 -C 4 alkyl, NHR, NR 2 , C(R a )═N—OR b , S(═O) p A 1 or C(═O)A 2 , or two radicals R 1 bound to adjacent carbon atoms can, together, also represent a group —O-Alk-O—, wherein Alk represents a linear or branched C 1 -C 4 alkylene, and 1, 2, 3 or 4 hydrogen atoms can also be replaced by halogen; R 2 represents C 1 -C 4 alkyl halide, C 1 -C 4 alkoxy, C 1 -C 4 alkoxy halide, hydroxy, halogen, CN or NO 2 ; whereby R 2 can also represent hydrogen or C 1 -C 4 alkyl when at least one of the three following conditions is fulfilled: n represents 3, 4 or 5; k represents 1, 2 or 3; if m is not equal to 0, at least one of the radicals R 1 represents a radical that differs from halogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy and C 1 -C 4 alkyl halide, and; R 3 represents C 1 -C 4 alkyl.