3-chloro-1-methylazetidine | 62999-27-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环丁烷
• 英文名称: 3-chloro-1-methylazetidine
• CAS: 62999-27-3
• 化学式: C₄H₈ClN
• 分子量: 105.567
• InChiKey: WXKCTFWSGGKULR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  6
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  3-chloro-1-methylazetidine 、 二苯乙腈 以 甲苯 为溶剂， 以6.7 g (27%)的产率得到(1-methyl-azetidin-3-yl)-diphenyl-acetonitrile
  参考文献：
  名称：

  Azetidinyl acetonitrile and acetamide antiarrhythmia compositions and

  摘要：

  以下化学式代表的.alpha.-(1-R-3-吡嗪基)-.alpha.-苯基-.alpha.-取代醯胺和-乙腈，其中R代表氢、低烷基、低环烷基或苯基低烷基，R.sup.1代表苯基或2-吡啶基，Y为具有抗心律失常活性的羰胺基或氰基。该发明还包括所述自由碱的药用可接受的酸盐和季铵盐。

  公开号：

  US04133881A1

文献信息

• Heterocyclic analgetic and antidiarrheal compounds
  申请人：A. H. Robins Company, Incorporated

  公开号：US04120969A1

  公开（公告）日：1978-10-17

  1-R-4-(omega-substituted alkyl)-3,3-diphenyl-2-pyrrolidinones of the formula ##STR1## wherein R is hydrogen, lower alkyl, cyclohexyl or benzyl, R.sup.1 is hydrogen, chloro, bromo, fluoro, trifluoromethyl or lower alkoxy, R.sup.2 is hydrogen, chloro, bromo, or fluoro, A is hydroxy, lower-alkylcarbonyloxy or lower-alkoxycarbonyl and n is 1, 2 or 3 having analgetic and antidiarrheal activity are disclosed. The pharmaceutically acceptable acid addition salts of the bases are within the scope of the present invention.

  1-R-4-(ω-取代烷基)-3,3-二苯基-2-吡咯烷酮，其通式如上所示，其中R为氢、低级烷基、环己基或苄基，R1为氢、氯、溴、氟、三氟甲基或低级烷氧基，R2为氢、氯、溴或氟，A为羟基、低级烷基羰氧基或低级烷氧基羰基，n为1、2或3，具有镇痛和止泻活性。本发明还涉及这些化合物的药用可接受的酸加成盐。
• 4-Hydroxymethyl-2-pyrrolidinones
  申请人：A. H. Robins Company, Inc.

  公开号：US04119637A1

  公开（公告）日：1978-10-10

  1-Hydrocarbon-3,3-diphenyl-4-hydroxymethyl-2-pyrrolidinones and methods for making them from 4,5-dihydro-3,3-diphenyl-4-hydrocarbylaminomethylfuran-2(3H)ones are disclosed. Methods for making the 4,5-dihydro-3,3-diphenyl-4-hydrocarbylaminomethylfuran-2(3H)ones are also disclosed. The novel compounds are useful intermediates for the preparation of pharmacologically active 4-(4,4-disubstitutedpiperidinylmethyl)-3,3-diphenyl-2-pyrrolidinones.

  本发明揭示了从4,5-二氢-3,3-二苯基-4-羟基甲基-2-吡咯烷酮衍生出1-烃基-3,3-二苯基-4-羟甲基-2-吡咯烷酮的方法。本发明还揭示了制备4,5-二氢-3,3-二苯基-4-烃基氨甲基呋喃-2（3H）酮的方法。这些新化合物是制备具有药理活性的4-(4,4-二取代哌啶基甲基)-3,3-二苯基-2-吡咯烷酮的有用中间体。
• 3-Methyleneazetidine derivatives
  申请人：A. H. Robins Company, Inc.

  公开号：US04260606A1

  公开（公告）日：1981-04-07

  This invention provides a novel class of 3-methyleneazetidines which include diphenylmethyl derivatives such as 1-isopropyl-3-diphenylmethyleneazetidine oxalate: ##STR1## This illustrated 3-methyleneazetidine compound is characterized by a combination of pharmacological properties which are indicative of utility as a mood elevating therapeutic agent for relieving the symptoms of depression in humans. The illustrated compound exhibits an ED.sub.50 (tetrabenazine-induced ptosis) of 2.18 mg/kg in mice.

  这项发明提供了一种新的3-亚甲基氮杂环化合物类，其中包括二苯甲基衍生物，如1-异丙基-3-二苯甲基氮杂环乙二酸盐：##STR1## 这种展示的3-亚甲基氮杂环化合物的特点是具有一种药理学性质的组合，表明其作为一种情绪提升的治疗剂在缓解人类抑郁症状方面具有实用性。这种展示的化合物在小鼠中表现出ED.sub.50（四苯丙嗪诱导的眼睑下垂）为2.18mg/kg。
• CALE, A. D. ,, JR.
  作者：CALE, A. D. ,, JR.

  DOI：——

  日期：——
• Azetidinyl acetonitrile and acetamide antiarrhythmia compositions and
  申请人：A. H. Robins Company, Incorporated

  公开号：US04133881A1

  公开（公告）日：1979-01-09

  .alpha.-(1-R-3-Azetidinyl)-.alpha.-phenyl-.alpha.-substituted-acetamides and -acetonitriles represented by the following formula: ##STR1## wherein R represents hydrogen, lower alkyl, lower cycloalkyl or phenyllower alkyl, R.sup.1 represents phenyl or 2-pyridyl, and Y is carbamoyl or cyano having antiarrhythmic activity are disclosed. Pharmaceutically acceptable acid addition salts of the free bases and quaternary salts are included as part of the invention.

  以下化学式代表的.alpha.-(1-R-3-吡嗪基)-.alpha.-苯基-.alpha.-取代醯胺和-乙腈，其中R代表氢、低烷基、低环烷基或苯基低烷基，R.sup.1代表苯基或2-吡啶基，Y为具有抗心律失常活性的羰胺基或氰基。该发明还包括所述自由碱的药用可接受的酸盐和季铵盐。