2-氨基-1-(2,5-二甲氧基苯基)乙酮 | 784138-79-0

• 中文名称: 2-氨基-1-(2,5-二甲氧基苯基)乙酮
• 英文名称: 2-amino-1-(2,5-dimethoxyphenyl) ethane-1-one
• 英文别名: 2-Amino-1-(2,5-dimethoxyphenyl)ethanone
• CAS: 784138-79-0
• 化学式: C₁₀H₁₃NO₃
• 分子量: 195.218
• InChiKey: IQFIJLKOVJRFBW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  61.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-氨基-1-(2,5-二甲氧基苯基)乙酮 在 sodium tetrahydroborate 、 sodium hydroxide 作用下， 以 甲醇 、 水 为溶剂， 反应 1.0h， 生成 2-氨基-1-(2,5-二甲氧基苯基)乙醇
  参考文献：
  名称：

  PROCESS FOR PREPARATION OF MIDODRINE AND INTERMEDIATES THEREOF

  摘要：

  该发明涉及制备米多吡啶或其药用可接受盐的过程。该发明还涉及制备米多吡啶中间体的过程。

  公开号：

  US20220144754A1
• 作为产物：
  描述：

  2-[2-(2,5-dimethoxyphenyl)-2-oxoethyl]-1H-isoindole-1,3(2H)-dione 在 盐酸 、 一水合肼 作用下， 生成 2-氨基-1-(2,5-二甲氧基苯基)乙酮
  参考文献：
  名称：

  PROCESS FOR PREPARATION OF MIDODRINE AND INTERMEDIATES THEREOF

  摘要：

  该发明涉及制备米多吡啶或其药用可接受盐的过程。该发明还涉及制备米多吡啶中间体的过程。

  公开号：

  US20220144754A1

文献信息

• [EN] AN IMPROVED PROCESS FOR THE SYNTHESIS OF (+/-) 2-AMINO-N-[2,(S,5-DIMETHOXYPHENYL)-2-HYDROXYETHYL] ACETAMIDE MONOHYDROCHLORIDE<br/>[FR] PROCESSUS DE SYNTHESE AMELIORE DE (+/-) 2-AMINO-N-[2,(S,5-DIMETHOXYPHENYL)-2-HYDROXYETHYL] ACETAMIDE MONOHYDROCHLORURE
  申请人：SANMAR SPECIALITY CHEMICALS LT

  公开号：WO2004018409A1

  公开（公告）日：2004-03-04

  This invention relates to an improved process for synthesizing (±) 2-Amino-N-[2,(S,5-dimethoxyphenyl)-2-hydroxyethyl] acetamide monohydrochloride in good yield and in a cost effective manner from 1-(2,5dimethoxyphenyl)-2-bromoethanone by reacting the same with hexamine in the presence of novel solvent system comprising Tetrahydrofuran and water. The resulting aminoethanone is acylated with haloacetylchloride and sodium acetate in acetone-water solvent system. This product is reduced selectively first with sodium borohydride and subsequently with stannous chloride. This product is converted in situ to the corresponding hydrochloride salt immediately after reduction on its own.

  这项发明涉及一种改进的工艺，用于从1-(2,5-二甲氧基苯基)-2-溴乙酮与六胺在包含四氢呋喃和水的新型溶剂体系中反应，以高产率和经济有效的方式合成（±）2-氨基-N-[2-（S，5-二甲氧基苯基）-2-羟乙基]乙酰胺单盐酸盐。所得的氨基乙酮在乙酮-水溶剂体系中与卤代乙酰氯和醋酸钠酰化。这种产物首先选择性地用硼氢化钠还原，随后用氯化亚锡还原。该产物在还原后自行立即转化为相应的盐酸盐。
• Process for the synthesis of (+) 2-amino-n-&lcub;2, (2,5-dimethoxy phenyl)-2-hydroxyethyl&rcub; acetamide monohydrochloride
  申请人：——

  公开号：US20040198836A1

  公开（公告）日：2004-10-07

  This invention relates to an improved process for synthesizing (±)-2-Amino-N-[2-(2,5-dimethoxyphenyl]-2-hydroxyethyl acetamide monohydrochloride in good yield and in a cost effective manner from 1-(2,5-dimethoxyphenyl)-2-bromoethanone by reacting the same with hexamine in the presence of novel solvent system comprising Tetrahydrofuran and water. The resulting aminoethanone is acylated with haloacetylchloride and sodium acetate in acetone-water solvent system. This product is reduced selectively first with sodium borohydride and subsequently with stannous chloride. This product is converted in situ to the corresponding hydrochloride salt immediately after reduction on its own.

  本发明涉及一种改进的工艺，可以从1-(2,5-二甲氧基苯基)-2-溴乙酮中，在新的溶剂体系Tetrahydrofuran和水的存在下，与六胺反应，以良好的产率和成本效益的方式合成(±)-2-氨基-N-[2-(2,5-二甲氧基苯基)-2-羟乙酰胺单盐酸盐。所得的氨基乙酮在乙酮-水溶剂体系中与卤代乙酰氯和醋酸钠酰化。该产物首先选择性地用硼氢化钠还原，然后再用氯化亚锡还原。该产物在还原后立即原位转化为相应的盐酸盐。
• HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS, IN PARTICULAR AS ANTI-ALZHEIMER AGENTS
  申请人：Marsais Francis

  公开号：US20090062279A1

  公开（公告）日：2009-03-05

  The invention is related to compound which comprises at least one radical C═Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C═Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease.

  本发明涉及一种化合物，其包含至少一个基团C═Y，其中Y为O或S，以及一个可氧化且不可质子化的氮原子N，其中在氧化时，基团C═Y的至少一个碳原子与氮原子之间的距离(d)在0.3至0.8纳米之间。本发明涉及由公式G定义的新杂环化合物及其制备方法，涉及包含它们的制药组合物以及它们在治疗神经退行性或阿尔茨海默病方面的用途。
• New heterocyclic compounds, their preparation and their use as medicaments, in particular as anti-alzheimer agents
  申请人：Institut National des Sciences Appliquees de Rouen (INSA)

  公开号：EP1731507A1

  公开（公告）日：2006-12-13

  The invention is related to compound which comprises at least one radical C=Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C=Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease.

  本发明涉及由至少一个基团C=Y（Y为O或S）和一个可氧化且不可质子化的氮原子N组成的化合物，其中基团C=Y的至少一个碳原子与氮原子之间的距离（d）在氧化时介于0.3至0.8纳米之间。 本发明涉及由式 G 定义的新杂环化合物、 它们的制备、包含它们的药物组合物以及它们作为治疗剂的用途，特别是在治疗神经退行性疾病或阿尔茨海默病中的用途。
• Imidazole and thiazole compositions for modifying biological signaling
  申请人：Ohio University

  公开号：US10023567B2

  公开（公告）日：2018-07-17

  Compounds having General Formula (I) or General Formula (II): in which R1 is chosen from C1 to C10 aliphatic or heteroaliphatic groups, optionally substituted with one or more aryl groups, substituted aryl groups, heteroaryl groups, substituted heteroaryl groups, or combination thereof; R2 is chosen from aromatic moieties, substituted aromatic moieties, heteroaromatic moieties substituted heteroaromatic moieties, and coumarin; R3 is chosen from —H, C1 to C10 aliphatic or heteroaliphatic groups, phenyl, or substituted phenyl, wherein the aliphatic or heteroaliphatic groups are optionally substituted with one or more phenyl groups, aryl groups, heteroaryl groups, substituted heteroaryl groups, or combination thereof, and wherein the aliphatic or heteroaliphatic groups are optionally bonded to R2 to form a ring; X is S or O; and Y is S or NH, may be used in pharmaceutical compositions that modify of biological signaling processes or as reagents for biological assays.

  具有通式(I)或通式(II)的化合物：其中 R1 选自 C1 至 C10 脂肪族或杂脂肪族基团，任选被一个或多个芳基、取代芳基、杂芳基、取代杂芳基或其组合取代；R2 选自芳香族基团、取代芳香族基团、杂芳香族基团、取代杂芳香族基团和香豆素；R3 选自-H、C1 至 C10 脂肪族或杂脂肪族基团、苯基或取代苯基，其中脂肪族或杂脂肪族基团可选择被一个或多个苯基、芳基、杂芳基、取代杂芳基或其组合取代，并且其中脂肪族或杂脂肪族基团可选择与 R2 键合形成环；X 是 S 或 O；Y 是 S 或 NH，可用于改变生物信号转导过程的药物组合物或用作生物检测试剂。