4-(2-chloro-4-methylphenyl)morpholine | 1444744-47-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 恶嗪烷类
• 英文名称: 4-(2-chloro-4-methylphenyl)morpholine
• CAS: 1444744-47-1
• 化学式: C₁₁H₁₄ClNO
• 分子量: 211.691
• InChiKey: MPTVSCITGCCNDM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  n-氯吗啉 、 三氟甲烷磺酸4-甲基-2-(三甲基硅基)苯酯 在 cesium fluoride 作用下， 以 乙腈 为溶剂， 生成 4-(2-chloro-5-methylphenyl)morpholine 、 4-(2-chloro-4-methylphenyl)morpholine
  参考文献：
  名称：

  Insertion of Arynes into N-Halo Bonds: A Direct Approach to o-Haloaminoarenes

  摘要：

  A new approach to access o-haloaminoarenes has been achieved by insertion of arynes into a nitrogen-halide bond (N-X). This transition-metal-free transformation displays a broad substrate scope of arynes, good compatibility with functional groups, and high regioselectivity. Representative transformations of the o-haloaminoarenes are described to highlight their utility for rapid access to diversely functionalized a minoarene derivatives.

  DOI：

  10.1021/ol401518c

文献信息

• NOVEL COMPOUNDS
  申请人：HALSALL Christopher Thomas

  公开号：US20080009482A1

  公开（公告）日：2008-01-10

  There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.

  提供了一个化合物的化学式(I)： 其制备方法，药物组合物以及在治疗中的用途。
• PYRIMIDINE DERIVATIVES
  申请人：Kettle Jason Grant

  公开号：US20110046108A1

  公开（公告）日：2011-02-24

  The invention concerns benzamide compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R 1 , ring A, n, R 3 , and R 4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4, and/or EphA2 and/or Src kinases.

  这项发明涉及Formula (I)的苯甲酰胺化合物或其药用可接受的盐，其中R1、环A、n、R3和R4如描述中所定义。本发明还涉及制备这种化合物的方法、含有它们的药物组合物以及它们在制造用作抗增殖剂的药物中的用途，用于预防或治疗对EphB4、EphA2和/或Src激酶抑制敏感的肿瘤或其他增殖病症。
• NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
  申请人：NAGARATHNAM Dhanapalan

  公开号：US20120289496A1

  公开（公告）日：2012-11-15

  The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

  本发明提供了PI3K蛋白激酶调节剂，其制备方法，含有它们的药物组合物，以及使用它们进行治疗、预防和/或改善激酶介导的疾病或紊乱的方法。
• Sulfopyrroles
  申请人：Eberle Martin

  公开号：US20070060570A1

  公开（公告）日：2007-03-15

  The invention relates to compounds of formula (I) wherein R 1 represents aryl, aralkyl or heteroaryl, R 2 is aryl or heteroaryl and R 3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.

  本发明涉及式(I)化合物，其中R1代表芳基、芳基烷基或杂芳基，R2为芳基或杂芳基，R3为芳基、杂芳基或可选取代的氨甲基；本发明还涉及合成这类化合物的方法，含有式(I)化合物的制药组合物，使用式(I)化合物制备用于治疗肿瘤和自身免疫性疾病的制药组合物，以及使用式(I)化合物或含有其的制药组合物治疗肿瘤和自身免疫性疾病的方法。
• IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
  申请人：Trabanco-Suarez Andres Avelino

  公开号：US20110009441A1

  公开（公告）日：2011-01-13

  The present invention relates to novel compounds, in particular novel imidazo[1,2-a]piridine derivatives according to Formula (I). The compounds according to the invention are positive allosteric modulators of metabotropic receptors-sub-type 2 (‘mGluR2’) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.

  本发明涉及新型化合物，特别是公式（I）中的新型咪唑并[1,2-a]吡啶衍生物。本发明的化合物是代谢型受体亚型2（“mGluR2”）的阳性变构调节剂，可用于治疗或预防与谷氨酸功能障碍有关的神经和精神障碍以及涉及代谢型受体亚型mGluR2的疾病。特别是，这些疾病是来自焦虑、精神分裂症、偏头痛、抑郁症和癫痫等中枢神经系统疾病的群体。本发明还涉及制备这些化合物和组合物的制药组合物和制备过程，以及将这些化合物用于预防和治疗涉及mGluR2的这些疾病的用途。