di-L-(+)-tartrate salt of (S)-2-aminomethyl-1-ethylpyrrolidine | 113310-91-1

• 分子结构分类: 有机化合物
• 英文名称: di-L-(+)-tartrate salt of (S)-2-aminomethyl-1-ethylpyrrolidine
• 英文别名: (R)-(+)-2-(aminomethyl)-1-ethylpyrrolidine (+)-ditartrate；R-(+)-2-aminomethyl-1-ethylpyrrolidine ditartrate
• CAS: 113310-91-1
• 化学式: 2C₄H₆O₆*C₇H₁₆N₂
• 分子量: 428.394
• InChiKey: TYOUPXABLTXXGB-OGFXRTJISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.69
• 重原子数：
  19.0
• 可旋转键数：
  5.0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.82
• 拓扑面积：
  144.32
• 氢给体数：
  5.0
• 氢受体数：
  6.0

反应信息

• 作为反应物：
  描述：

  3-溴-2,6-二甲氧基苯甲酰氯 、 di-L-(+)-tartrate salt of (S)-2-aminomethyl-1-ethylpyrrolidine 在 sodium hydroxide 作用下， 以 氯仿 为溶剂， 反应 0.17h， 生成 (R)-(+)-2-[(3-bromo-2,6-dimethoxybenzamido)methyl]-1-ethylpyrrolidine
  参考文献：
  名称：

  Potential neuroleptic agents. 2,6-Dialkoxybenzamide derivatives with potent dopamine receptor blocking activities

  摘要：

  A series of some novel N-(l-ethyl-2-pyrrolidinylmethyl)benzamides was synthesized and tested for dopamine receptor blockade in vivo by the ability to block the apomorphine syndrome in the rat. Several compounds were considerably more potent than sulpiride as dopamine receptor blockers and displayed low liability to induce extrapyramidal side effects (catalepsy) in the rat. The blockade of dopamine receptor activity in vivo was mainly confined to the levorotatory isomers having the S absolute configuration. The structure-activity relationships are discussed.

  DOI：

  10.1021/jm00353a003

文献信息

• 4-Quinolinylamino-N-[pyrrolidinyl or
  申请人：American Home Products Corporation

  公开号：US04695574A1

  公开（公告）日：1987-09-22

  4-Aminoquioline derivatives having the formula ##STR1## and their pharmaceutically acceptable salts where X.sub.1 is halogen or trifluoromethyl and X.sub.2 is a group having the formula --NR.sub.1 --Q--N--R.sub.4 (II) where R.sub.1 is hydrogen or lower alkyl; Q is lower alkylene; R.sub.4 is lower alkyl and the ring illustrated is a piperidine or pyrrolidine ring optionally substituted by lower alkyl, exhibit anti-hypertensive activity. Corresponding compounds where R.sub.4 is replaced by latent lower alkyl, a protecting group or hydrogen may be used as intermediates.

  具有以下结构式的4-氨基喹啉衍生物及其药用可接受的盐，其中X.sub.1是卤素或三氟甲基，X.sub.2是具有以下结构式的基团--NR.sub.1 --Q--N--R.sub.4 (II)，其中R.sub.1是氢或较低的烷基；Q是较低的烷基；R.sub.4是较低的烷基，所示环是一个哌啶或吡咯烷环，可以选择地被较低的烷基取代，具有抗高血压活性。相应的化合物，其中R.sub.4被取代为潜隐的较低烷基、保护基或氢，可用作中间体。