5-(2-Methoxy-4-nitrophenyl)-4-methyloxazole | 1239719-43-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-(2-Methoxy-4-nitrophenyl)-4-methyloxazole
• 英文别名: 5-(2-methoxy-4-nitrophenyl)-4-methyl-1,3-oxazole
• CAS: 1239719-43-7
• 化学式: C₁₁H₁₀N₂O₄
• 分子量: 234.211
• InChiKey: OFJDUBHZMDGNPX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  81.1
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5-(2-Methoxy-4-nitrophenyl)-4-methyloxazole 在 palladium 10% on activated carbon 噻吩 、 氢气 作用下， 以 甲醇 、 异丙醚 为溶剂， 以99%的产率得到3-methoxy-4-(4-methyloxazol-5-yl)aniline
  参考文献：
  名称：

  [EN] NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
  [FR] NOUVEAUX DÉRIVÉS DE TRIAZOLE SUBSTITUÉS COMME MODULATEURS DE GAMMA SECRÉTASE

  摘要：

  本发明涉及一种新型的Formula (I)中的取代三唑衍生物，其中Het1、R1、R2、A1、A2、A3、A4、L1和L2的含义如权利要求中所定义。根据本发明的化合物可用作γ-分泌酶调节剂。本发明还涉及制备这种新型化合物的方法，包括将所述化合物作为活性成分的药物组合物以及将所述化合物用作药物的用途。

  公开号：

  WO2011086099A1
• 作为产物：
  描述：

  2-甲氧基-4-硝基苯甲醛 、 1-甲基-对甲苯磺酰甲基异腈 在 potassium carbonate 作用下， 以 甲醇 为溶剂， 反应 4.0h， 以77%的产率得到5-(2-Methoxy-4-nitrophenyl)-4-methyloxazole
  参考文献：
  名称：

  NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS

  摘要：

  本发明涉及具有以下式（I）的新型取代三唑衍生物，其中Het1，R1，R2，A1，A2，A3，A4，L1和L2的含义如权利要求中所定义。根据本发明的化合物可用作γ-分泌酶调节剂。本发明还涉及制备这种新型化合物的方法，包括将所述化合物作为活性成分的药物组合物以及将所述化合物用作药物的用途。

  公开号：

  US20120295891A1

文献信息

• [EN] NOVEL SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS GAMMA SECRETASE MODULATORS<br/>[FR] NOUVEAUX COMPOSÉS HÉTÉROCYCLIQUES BICYCLIQUES SUBSTITUÉS EN TANT QUE MODULATEURS DE LA GAMMA-SÉCRÉTASE
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2010089292A1

  公开（公告）日：2010-08-12

  The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

  本发明涉及式（I）的取代双环杂环化合物，其中Het1、Het2、A1、A2、A3和A4的含义如权利要求中所定义。根据本发明的化合物可用作γ-分泌酶调节剂。本发明还涉及制备这种新化合物的方法，包含所述化合物作为活性成分的药物组合物，以及将所述化合物用作药物的用途。
• [EN] NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS<br/>[FR] NOUVEAUX DÉRIVÉS DE TRIAZOLE SUBSTITUÉS COMME MODULATEURS DE GAMMA SECRÉTASE
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2011086099A1

  公开（公告）日：2011-07-21

  The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

  本发明涉及一种新型的Formula (I)中的取代三唑衍生物，其中Het1、R1、R2、A1、A2、A3、A4、L1和L2的含义如权利要求中所定义。根据本发明的化合物可用作γ-分泌酶调节剂。本发明还涉及制备这种新型化合物的方法，包括将所述化合物作为活性成分的药物组合物以及将所述化合物用作药物的用途。
• [EN] NOVEL SUBSTITUTED BICYCLIC TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS<br/>[FR] NOUVEAUX DÉRIVÉS DE TRIAZOLE BICYCLIQUES SUBSTITUÉS COMME MODULATEURS DE GAMMA SECRÉTASE
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2011086098A1

  公开（公告）日：2011-07-21

  The present invention is concerned with novel substituted bicyclic triazole derivatives of Formula (I) wherein Het1, R1, R2, A1, A2, A3, A4, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

  本发明涉及一种新型的取代的Formula (I)中的双环三唑衍生物，其中Het1、R1、R2、A1、A2、A3、A4、L1和L2的含义如权利要求中所定义。根据本发明的化合物可用作γ-分泌酶调节剂。本发明还涉及制备这种新型化合物的方法，包括将所述化合物作为活性成分的药物组合物以及将所述化合物用作药物的用途。
• [EN] NOVEL SUBSTITUTED INDAZOLE AND AZA-INDAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS<br/>[FR] NOUVEAUX DÉRIVÉS SUBSTITUÉS D'INDAZOLE ET D'AZA-INDAZOLE UTILISÉS COMME MODULATEURS DE LA GAMMA SÉCRÉTASE
  申请人：ORTHO MCNEIL JANSSEN PHARM

  公开号：WO2010145883A1

  公开（公告）日：2010-12-23

  The present invention is concerned with novel substituted indazole and aza-indazole derivatives of Formula (I), wherein R1, R2, R3, R4, Y, A1, A2, A3, A4, X1, X2, X3 and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

  本发明涉及具有公式（I）中定义的R1、R2、R3、R4、Y、A1、A2、A3、A4、X1、X2、X3和Het1含义的新型取代的吲唑和氮杂吲唑衍生物。根据本发明的化合物可用作γ-分泌酶调节剂。该发明还涉及制备这种新型化合物的过程，包含该化合物作为活性成分的药物组合物以及将该化合物用作药物的用途。
• NOVEL SUBSTITUTED BICYCLIC HETEROCYCLIC COMPOUNDS AS GAMMA SECRETASE MODULATORS
  申请人：CELLZOME LIMITED

  公开号：US20150094311A1

  公开（公告）日：2015-04-02

  The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het 1 , Het 2 , A 1 , A 2 , A 3 and A 4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.