2,5-哌嗪二酮,1,3,4-三甲基-(9CI) | 298700-23-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 2,5-哌嗪二酮,1,3,4-三甲基-(9CI)
• 英文名称: (s)-Tolperisone
• 英文别名: (2S)-2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one
• CAS: 298700-23-9
• 化学式: C₁₆H₂₃NO
• 分子量: 245.36
• InChiKey: FSKFPVLPFLJRQB-AWEZNQCLSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  18
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• Method for producing salts of tolperisone
  申请人：Czollner Laszlo

  公开号：US20060041141A1

  公开（公告）日：2006-02-23

  The invention relates to a method for producing an addition salt of 2,4′-dimethyl-3-piperidino-propiophenone (tolperisone) with a pharmaceutically acceptable acid, of formula (I). According to the invention, 4-methylpropiophenone is reacted with piperidine hydrochloride and 1,2-dioxolane in the presence of an acid serving as a catalyst, and the tolperisone obtained in the form of an acid addition salt is separated by filtering after the reaction mixture has cooled down.

  本发明涉及一种制备2,4'-二甲基-3-哌嗪基丙酮酸加成盐（托尔哌酮）的药物可接受酸的方法，其化学式为（I）。根据本发明，将4-甲基丙酮酸与盐酸哌啶和1,2-二氧兰在催化剂作用下反应，反应混合物冷却后通过过滤分离得到托尔哌酮的酸加成盐。
• Addition Salts of Tolperisone, Processes for Their Preparation and Use Thereof
  申请人：Alken Rudolf-Giesbert

  公开号：US20090298893A1

  公开（公告）日：2009-12-03

  Addition salts of 2,4′-dimethyl-3-piperidinopropiophenone (tolperisone) are described, wherein the salt is formed with an acid R—COOH and wherein R is the organic group of a physiologically compatible organic acid. Described also are processes for the preparation of these addition salts, the use thereof for pharmaceutical preparations and pharmaceuticals containing these addition salts.

  本文描述了2,4'-二甲基-3-哌啶丙酮酸加成盐（托尔哌酮），其中盐是与酸R-COOH形成的，其中R是生理兼容有机酸的有机基团。还描述了制备这些加成盐的过程，以及将其用于制药制剂和含有这些加成盐的药物的用途。
• Method for administering tolperisone
  申请人：Bodenteich Angelika

  公开号：US20070249673A1

  公开（公告）日：2007-10-25

  The present invention is directed to methods of administering tolperisone (2,4′-dimethyl-3-piperidinopropiophenone; 1-propanone, 2-methyl-1-(4-methylphenyl)-3-(-piperidinyl)), and kits comprising the same.
• PROCESS FOR THE PRODUCTION OF HIGH-PURITY 2,4'-DIMETHYL-3-PIPERIDINO-PROPIOPHENONE (TOLPERISONE), PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THE LATTER, AS WELL AS ACTIVE INGREDIENT FORMULATIONS THAT CONTAIN TOLPERISONE
  申请人：Welzig Stefan

  公开号：US20100150995A1

  公开（公告）日：2010-06-17

  The invention relates to a method for producing highly pure 2,4′-dimethyl-3-piperidino-propiophenone (tolperisone) (formula I) and the pharmaceutically acceptable salts, hydrochlorides, and hydrates thereof. The method allows the content of the undesired byproduct 2-methyl-1-(4-methylphenyl) propenone (4-MMPPO) to be kept significantly lower than in previously known methods. The invention further relates to active substance formulations which contain tolperisone and are suitable, among other things, for producing combination preparations used for treating patients suffering from Alzheimer's disease. The invention also relates to topical formulations, controlled release (CR) formulations, and transdermal therapeutic systems, such as active substance patches, which contain less than 50 ppm, preferably less than 10 ppm, more preferably less than 7 ppm, and most preferably less than 3 ppm or 0 ppm (i.e. less than the detectable amount) of the undesired byproduct 2-methyl-1-(4-methylphenyl) propenone (4-MMPPO) in relation to 100 percent by weight of active substance.
• US7385060B2
  申请人：——

  公开号：US7385060B2

  公开（公告）日：2008-06-10