3-methoxy-4-(2-methyloxazol-5-yl)aniline | 568556-28-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 3-methoxy-4-(2-methyloxazol-5-yl)aniline
• 英文别名: 3-methoxy-4-(2-methyl-oxazol-5-yl)-phenylamine；3-Methoxy-4-(2-methyloxazol-5-yl)benzenamine；3-methoxy-4-(2-methyl-1,3-oxazol-5-yl)aniline
• CAS: 568556-28-5
• 化学式: C₁₁H₁₂N₂O₂
• 分子量: 204.228
• InChiKey: IITAIDUEQYLJJH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  15
• 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：
  61.3
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-benzyl-2-chloro-6-methyl-pyrimidine 、 3-methoxy-4-(2-methyloxazol-5-yl)aniline 在 palladium diacetate 、 2-(二环己基膦基)联苯 sodium t-butanolate 作用下， 以 1,4-二氧六环 为溶剂， 反应 0.5h， 以27%的产率得到(4-benzyl-6-methyl-pyrimidin-2-yl)-[3-methoxy-4-(2-methyl-oxazol-5-yl)-phenyl]-amine
  参考文献：
  名称：

  MODULATORS FOR AMYLOID BETA

  摘要：

  该发明涉及以下式的化合物 其中取代基如权利要求中所述 。式I的化合物是淀粉样蛋白β的调节剂，因此它们可能对治疗或预防与大脑中β-淀粉样蛋白沉积相关的疾病有用，特别是阿尔茨海默病，以及其他疾病，如脑淀粉样血管病变，遗传性脑出血伴淀粉样变性，荷兰型（HCHWA-D），多梗死性痴呆，拳击性痴呆和唐氏综合征。

  公开号：

  US20090215759A1
• 作为产物：
  描述：

  Acetic acid (Z)-2-azido-1-(2-methoxy-4-nitro-phenyl)-vinyl ester 在 palladium on activated charcoal 氢气 、 亚磷酸三乙酯 作用下， 以 1,4-二氧六环 、 甲醇 为溶剂， 20.0~90.0 ℃ 、310.26 kPa 条件下， 反应 20.5h， 生成 3-methoxy-4-(2-methyloxazol-5-yl)aniline
  参考文献：
  名称：

  Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety

  摘要：

  The first reported structure-activity relationships (SARs) about the N-[3-methoxy-4-(5-oxazolyi)phenyl moiety for a series of recently disclosed inosine monophosphate dehydrogenase (IMPDH) inhibitors are described. The syntheses and in vitro inhibitory values for IMPDH II, and T-cell proliferation (for select analogues) are given. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00258-0

文献信息

• NOVEL SUBSTITUTED TRIAZOLE DERIVATIVES AS GAMMA SECRETASE MODULATORS
  申请人：Van Brandt Sven Franciscus Anna

  公开号：US20120295891A1

  公开（公告）日：2012-11-22

  The present invention is concerned with novel substituted triazole derivatives of Formula (I) wherein Het 1 , R 1 , R 2 , A 1 , A 2 , A 3 , A 4 , L 1 , and L 2 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。
• [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] PYRIMIDINE COMPOUNDS AND THEIR USE AS GAMMA SECRETASE MODULATORS<br/>[FR] COMPOSÉS DE PYRIMIDINE ET LEUR UTILISATION COMME MODULATEURS DE LA GAMMA-SÉCRÉTASE
  申请人：ACTURUM LIFE SCIENCE AB

  公开号：WO2014195323A1

  公开（公告）日：2014-12-11

  The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The invention also relates to pharmaceutical compositions comprising these compounds, to processes for making these compounds, and to their use as medicaments for treatment and/or prevention of Aβ-related diseases.

  本发明涉及式(I)化合物及其药用可接受的盐。该发明还涉及包含这些化合物的药物组合物，制造这些化合物的方法，以及它们作为治疗和/或预防Aβ相关疾病的药物的应用。
• [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。