(+/-)-1,4-dimethyl-3,3-diphenyl-2-pyrrolidone | 87274-96-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (+/-)-1,4-dimethyl-3,3-diphenyl-2-pyrrolidone
• 英文别名: 1,4-dimethyl-3,3-diphenyl-pyrrolidin-2-one；1,4-Dimethyl-3,3-diphenyl-pyrrolidin-2-on；1,4-Dimethyl-3,3-diphenyl-pyrrolid-2-on；1,4-Dimethyl-3,3-diphenyl-2-pyrrolidinone；1,4-dimethyl-3,3-diphenylpyrrolidin-2-one
• CAS: 87274-96-2
• 化学式: C₁₈H₁₉NO
• 分子量: 265.355
• InChiKey: ZPRNVLOIRXXUNY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  2-氯-N,N-二甲基-1-丙胺 在 盐酸 、 potassium tert-butylate 、 氢溴酸 、 亚硝酸 、 碳酸氢钠 作用下， 反应 24.0h， 生成 (+/-)-1,4-dimethyl-3,3-diphenyl-2-pyrrolidone
  参考文献：
  名称：

  3,3-二苯基-2-吡咯烷酮衍生物的合成和抗惊厥筛选。

  摘要：

  合成了6种3,3-二苯基-2-吡咯烷酮衍生物，并筛选了其抗惊厥活性。合成途径涉及中间体N，N-二甲基氨基腈与氯甲酸甲酯的单-N-去甲基化，然后将氨基甲酸酯基团裂解。在这六种衍生物中，（+/-）-2-亚氨基-1,5-二甲基-3,3-二苯基吡咯烷盐酸盐可有效保护小鼠免受最大电击（MES）诱发的癫痫发作（剂量为30 mg / kg） 。

  DOI：

  10.1002/jps.2600720627

文献信息

• 139. Search for new analgesics. Part III. Homologues of amidone, isoamidone, and some related compounds
  作者：E. Walton、P. Ofner、R. H. Thorp

  DOI：10.1039/jr9490000648

  日期：——
• Ocular toxicity study of trypan blue injected into the vitreous cavity of rabbit eyes
  作者：Marc Veckeneer、Koen Overdam、Jan Monzer、Karin Kobuch、Wilfried Marle、Henk Spekreijse、Jan Meurs

  DOI：10.1007/s004170100341

  日期：2001.9

  Background: To evaluate the ocular toxicity of trypan blue (TB) injected into the vitreous cavity of rabbit eyes. TB is a dye that could be useful for staining epiretinal membranes during vitrectomy surgery. Methods: Ten New Zealand White (NZW) rabbits underwent gas-compression vitrectomy. Rabbits were divided into three groups to receive injections of 0.1 ml basic salt solution, 0.1 ml of a 0.06% TB solution or 0.1 ml of a 0.2% TB solution. Ocular toxicity was assessed by slit-lamp biomicroscopy, ophthalmoscopy, electroretinography and histology. Results: Transient posterior capsule opacification was noted in all animals. No significant reductions in a-wave or b-wave amplitudes were found in any of the animals. Light and electron microscopic examination of the inferior retina in the 0.2% TB-treated eyes showed damaged photoreceptors and marked disorganization. Immunohistochemical staining for rhodopsin was strongly reduced in those sections and staining for proliferation with Ki-67 was positive. No histological abnormalities were found in the upper retina of the 0.2% TB-treated eyes or in any part of the retina of the 0.06% TB-treated or control eyes. No histological abnormalities were found in any of the anterior chamber angle specimens. Conclusions: Although no signs of toxicity were found after the prolonged presence of TB at a concentration of 0.06% in the vitreous cavity of rabbit eyes, marked damage occurred in the lower retina of 0.2% TB-treated eyes. The shortterm presence of TB at a concentration of 0.06% in the vitreous cavity is harmless to the rabbit eye but a higher concentration of TB could be unsafe.
• Some New Compounds Related to Amidone
  作者：John H. Gardner、Nelson R. Easton、Joseph R. Stevens

  DOI：10.1021/ja01189a022

  日期：1948.9
• PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATMENT OF PAIN
  申请人：Board Of Regents Of the University Of Texas System

  公开号：EP3468540A1

  公开（公告）日：2019-04-17
• [EN] PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATMENT OF PAIN<br/>[FR] COMPOSITIONS PHARMACEUTIQUES ET MÉTHODES DE TRAITEMENT DU CANCER
  申请人：UNIV TEXAS

  公开号：WO2017218518A1

  公开（公告）日：2017-12-21

  Compositions and methods for treatment of acute and chronic pain are disclosed herein. These compositions include fixed dose oral formulations containing an atypical antipsychotic drug and an opioid. Also provided here are methods of treatment of pain, particularly chronic pain while attenuating the abuse-liability of prescription pain medications.