3-乙基-4-(1H-吲哚-2-基)-5-甲基-1,2-恶唑 | 80565-40-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 中文名称: 3-乙基-4-(1H-吲哚-2-基)-5-甲基-1,2-恶唑
• 英文名称: 2-(3-ethyl-5-methyl-4-isoxazolyl)-indole
• 英文别名: 2-(3-Ethyl-5-methyl-1,2-oxazol-4-yl)-1H-indole；3-ethyl-4-(1H-indol-2-yl)-5-methyl-1,2-oxazole
• CAS: 80565-40-8
• 化学式: C₁₄H₁₄N₂O
• 分子量: 226.278
• InChiKey: GHCMPCIHNKLYIM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  41.8
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-乙基-4-(1H-吲哚-2-基)-5-甲基-1,2-恶唑 、 草酰氯 生成 2-[2-(3-ethyl-5-methyl-1,2-oxazol-4-yl)-1H-indol-3-yl]-2-oxoacetyl chloride
  参考文献：
  名称：

  NADELSON, J.;BRAND, L. J.

  摘要：

  DOI：
• 作为产物：
  描述：

  N-[(E)-1-(3-ethyl-5-methyl-1,2-oxazol-4-yl)ethylideneamino]aniline 生成 3-乙基-4-(1H-吲哚-2-基)-5-甲基-1,2-恶唑
  参考文献：
  名称：

  BRAND, L. J.;NADELSON, J.

  摘要：

  DOI：

文献信息

• 2-substituted-3-indolamines and use thereof as anti-diabetics
  申请人：Sandoz, Inc.

  公开号：US04582848A1

  公开（公告）日：1986-04-15

  This disclosure relates to substituted indolamines, which exhibit anti-diabetic activity, having the formula: ##STR1## where m is an integer from 1 to 4, x represents hydrogen or --OH R represents Ar or ##STR2## and Ar represents ##STR3## R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl or lower alkoxy, R.sub.2 and R.sub.3 each, independently, represent lower alkyl, or R.sub.2 and R.sub.3 together with N represent ##STR4## wherein n is 1, 2 or 3, R.sub.4 represents hydrogen or lower alkyl, and R.sub.5 represents hydrogen or lower alkyl, unsubstituted phenyl or phenyl substituted with fluoro, chloro, lower alkyl or lower alkoxy, or or pharmaceutically acceptable acid addition salts thereof.

  这项披露涉及取代吲哚胺，其具有抗糖尿病活性，其化学式为：##STR1##其中m是1到4之间的整数，x代表氢或--OH，R代表Ar或##STR2##，Ar代表##STR3##，R.sub.1代表氢、氟、氯、较低烷基或较低烷氧基，R.sub.2和R.sub.3各自独立地代表较低烷基，或R.sub.2和R.sub.3与N一起代表##STR4##其中n为1、2或3，R.sub.4代表氢或较低烷基，R.sub.5代表氢或较低烷基，未取代的苯基或苯基取代的氟、氯、较低烷基或较低烷氧基，或其药用可接受的酸盐。
• Isoxazolyl indolamines having anti-diabetic activity
  申请人：Sandoz, Inc.

  公开号：US04536499A1

  公开（公告）日：1985-08-20

  This disclosure describes novel compounds of the formula ##STR1## where m is 2, 3 or 4 X is hydrogen or hydroxy R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms or lower alkoxy having 1 to 4 carbon atoms, and R.sub.2 and R.sub.3 each independently represent lower alkyl as defined above, or R.sub.2 and R.sub.3 together with N represent ##STR2## wherein n is 1, 2 or 3, and R.sub.4 represents hydrogen or lower alkyl as defined above, and R.sub.5 represents hydrogen, lower alkyl, phenyl or phenyl substituted with fluoro, chloro, lower alkyl having 1 to 4 carbon atoms, or lower alkoxy having 1 to 4 carbon atoms, with the proviso that when X is hydroxy, m is 3 or 4, or a pharmaceutically acceptable acid addition salt thereof, which are useful in the treatment of diabetes by inhibiting or impeding post-prandial hyperglycemia.

  本公开描述了一种新颖的化合物，其化学式为##STR1##其中m为2、3或4，X为氢或羟基，R.sub.1代表氢、氟、氯、1至4个碳原子的低碳烷基或1至4个碳原子的低碳基氧基，R.sub.2和R.sub.3分别独立地代表如上定义的低碳烷基，或R.sub.2和R.sub.3与N一起代表##STR2##其中n为1、2或3，R.sub.4代表氢或如上定义的低碳烷基，R.sub.5代表氢、低碳基、苯基或苯基取代的氟、氯、1至4个碳原子的低碳烷基或1至4个碳原子的低碳基氧基，但当X为羟基时，m为3或4，或其药学上可接受的酸盐，这些化合物在通过抑制或阻碍餐后高血糖症治疗糖尿病方面具有用处。
• Isoxazolyl indolamines
  申请人：Sandoz, Inc.

  公开号：US04336379A1

  公开（公告）日：1982-06-22

  This disclosure describes compounds of the formula ##STR1## where R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms or lower alkoxy having 1 to 4 carbon atoms, and R.sub.2 represents hydroxy, and R.sub.3 and R.sub.4 each independently represent lower alkyl as defined above, or R.sub.3 and R.sub.4 together with N represent ##STR2## wherein n is 1, 2 or 3, and R.sub.5 and R.sub.6 each independently represent hydrogen or lower alkyl as defined above, or a pharmaceutically acceptable acid addition salt thereof, which are useful as anti-diabetic agents, in particular as hypoglycemic agents and inhibiting or impeding post-prandial hyperglycemia.

  本公开描述了以下结构的化合物##STR1##其中R.sub.1代表氢、氟、氯、具有1至4个碳原子的低碳烷基或具有1至4个碳原子的低碳氧基，R.sub.2代表羟基，R.sub.3和R.sub.4各自独立地代表如上所定义的低碳烷基，或R.sub.3和R.sub.4与N一起代表##STR2##其中n为1、2或3，R.sub.5和R.sub.6各自独立地代表氢或如上所定义的低碳烷基，或其药学上可接受的酸盐，这些化合物可用作抗糖尿病药物，特别是作为降糖药物，用于抑制或阻碍餐后高血糖。
• Isoxazolyl indolamines as hypoglycemics
  申请人：Sandoz, Inc.

  公开号：US04421752A1

  公开（公告）日：1983-12-20

  This disclosure describes compounds of the formula ##STR1## where R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms or lower alkoxy having 1 to 4 carbon atoms, and R.sub.2 and R.sub.3 each independently represent lower alkyl as defined above, or R.sub.2 and R.sub.3 together with N represent ##STR2## wherein n is 1, 2 or 3, and R.sub.4 and R.sub.5 each independently represent hydrogen or lower alkyl as defined above, or a pharmaceutically acceptable acid addition salt thereof, which are useful as anti-diabetic agents in particular as hypoglycemic agents and inhibiting or impeding post-prandial hyperglycemia.

  本公开说明了以下式子的化合物：##STR1## 其中，R.sub.1代表氢、氟、氯、具有1至4个碳原子的低级烷基或具有1至4个碳原子的低级烷氧基，而R.sub.2和R.sub.3各自独立地代表如上所定义的低级烷基，或者R.sub.2和R.sub.3与N一起代表##STR2## 其中n为1、2或3，而R.sub.4和R.sub.5各自独立地代表氢或者如上所定义的低级烷基，或其药学上可接受的酸加成盐。这些化合物可用作抗糖尿病药物，特别是作为降血糖药物，并能够抑制或阻碍餐后高血糖。
• Isoxazolyl indolamines for treating diabetes
  申请人：Sandoz, Inc.

  公开号：US04415568A1

  公开（公告）日：1983-11-15

  This disclosure describes compounds of the formula ##STR1## wherein R.sub.1 represents hydrogen, fluoro, chloro, lower alkyl having 1 to 4 carbon atoms, or lower alkoxy having 1 to 4 carbon atoms, and R.sub.2 represents lower alkyl or ##STR2## where R.sub.5 represents hydrogen, fluoro, chloro, lower alkyl or lower alkoxy, and R.sub.3 and R.sub.4 each independently represent lower alkyl as defined above, and R.sub.3 and R.sub.4 together with N represent ##STR3## or pharmaceutically acceptable acid addition salts thereof, which are useful as anti-diabetic agents.

  本公开说明了以下式子的化合物：##STR1## 其中R.sub.1代表氢、氟、氯、1到4个碳原子的低碳基或1到4个碳原子的低碳氧基，R.sub.2代表低碳基或##STR2## 其中R.sub.5代表氢、氟、氯、低碳基或低碳氧基，R.sub.3和R.sub.4各自独立地代表如上定义的低碳基，而R.sub.3和R.sub.4与N一起代表##STR3## 或其药学上可接受的酸加盐，其作为抗糖尿病药物具有用途。