1,1,N-trimethyl-N-(3,3-diphenylpropyl)-2-aminoethyl α-acetyl-3-nitrocinnamate | 100427-53-0

• 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: 1,1,N-trimethyl-N-(3,3-diphenylpropyl)-2-aminoethyl α-acetyl-3-nitrocinnamate
• 英文别名: 1-((3,3-Diphenylpropyl)(methyl)amino)-2-methylpropan-2-yl 2-(3-nitrobenzylidene)-3-oxobutanoate；[1-[3,3-diphenylpropyl(methyl)amino]-2-methylpropan-2-yl] (2E)-2-[(3-nitrophenyl)methylidene]-3-oxobutanoate
• CAS: 100427-53-0
• 化学式: C₃₁H₃₄N₂O₅
• 分子量: 514.621
• InChiKey: BCYDMCYQBTZFDU-XHLNEMQHSA-N

物化性质

• 沸点：
  645.6±55.0 °C(Predicted)
• 密度：
  1.170±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  6.3
• 重原子数：
  38
• 可旋转键数：
  12
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  92.4
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  1,1,N-trimethyl-N-(3,3-diphenylpropyl)-2-aminoethyl α-acetyl-3-nitrocinnamate 、 β-氨基巴豆酸甲酯 以 异丙醇 为溶剂， 反应 3.0h， 生成 乐卡地平
  参考文献：
  名称：

  Solid lercanidipine free base

  摘要：

  本发明提供了基本纯度为至少95％，优选至少97％，更优选至少99％，还更优选至少99.5％的左旋卡尼地平游离基。本发明的左旋卡尼地平游离基以非晶态固体形式形成，易于处理，特别适用于制药组合物的制备。

  公开号：

  US20060199849A1

文献信息

• NOVEL PROCESS FOR THE PREPARATION OF LERCANIDIPINE
  申请人：Parthasaradhi Reddy Bandi

  公开号：US20090227800A1

  公开（公告）日：2009-09-10

  The invention provides a novel process for the preparation of lercanidipine or a pharmaceutical acceptable salt using novel intermediates. Thus, 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol is reacted with trimethylsilyl chloride in presence of triethyl amine in methylene chloride to give 2,N-dimethyl-2-(trimethylsilyloxy)-N-(3,3-diphenylpropyl)-1-propanamine, which is then reacted with 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carbonyl chloride for 2 hours and crystallized to obtain lercanidipine hydrochloride.

  本发明提供了一种使用新型中间体制备lercanidipine或药用可接受盐的新工艺。因此，2，N-二甲基-N-(3,3-二苯基丙基)-1-氨基-2-丙醇在三乙胺存在下与三甲基氯硅烷反应，在甲基氯中生成2，N-二甲基-2-(三甲基硅氧基)-N-(3,3-二苯基丙基)-1-丙胺，然后与2,6-二甲基-5-甲氧羰基-4-(3-硝基苯基)-1,4-二氢吡啶-3-羧酰氯反应2小时，并结晶得到lercanidipine盐酸盐。
• Lercanidipine Hydrochloride Polymorphs and an Improved Process for Preparation of 1,1,N-Trimethyl-N-(3,3-Diphenylpropyl)-2-Aminoethyl Acetoacetate
  申请人：Dixit Girish

  公开号：US20100104649A1

  公开（公告）日：2010-04-29

  Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of substantially pure Lercanidipine intermediate, 1,1,N-trimethyl-N-(3,3-diphenylpropyl)-2-aminoethyl acetoacetate. The intermediate is useful for preparing Lercanidipine, or a pharmaceutically acceptable salt thereof, in high yield and purity. The present invention further provides a novel crystalline form of Lercanidipine hydrochloride and a process for its preparation. The present invention also provides a process for the preparation of amorphous form of Lercanidipine hydrochloride.

  本文公开了一种改进的、商业可行的和工业上有利的制备基本纯Lercanidipine中间体1,1,N-三甲基-N-(3,3-二苯基丙基)-2-氨基乙酰乙酸酯的方法。该中间体可用于高收率和高纯度地制备Lercanidipine或其药学上可接受的盐。本发明还提供了一种新的晶体形式的Lercanidipine盐酸盐及其制备方法。本发明还提供了一种制备Lercanidipine盐酸盐无定形形式的方法。
• Asymmetrical diesters of 1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylic acid
  申请人：RECORDATI S.A. CHEMICAL and PHARMACEUTICAL COMPANY

  公开号：EP0153016A2

  公开（公告）日：1985-08-28

  Compounds I (Ph = phenyl; Ar = 2 - nitrophenyl, 3-nitrophenyl, 2,3-dichlorphenyl or benzofurazan-4-yl; A = C2 - C6 alkylene; R = C1 - C6 alkyl optionally C1 - C6 alkoxy monosubstituted; R1 = H, OH or C1- C4 alkyl; R2 = H or CH3) have antihypertensive activity and are effective against coronary heart diseases. They are prepared starting from the aldehyde ArCHO and esters of acetoacetic acid and 3-amino-crotonic acid. Pharmaceutical preparations containing them are also described.

  化合物 I（Ph =苯基；Ar = 2-硝基苯基、3-硝基苯基、2,3-二氯苯基或苯并呋咱-4-基；A = C2 - C6 亚烷基；R = C1 - C6 烷基，可选 C1 - C6 烷氧基单取代；R1 = H、OH 或 C1 - C4 烷基；R2 = H 或 CH3）具有抗高血压活性，对冠心病有效。 它们是由醛 ArCHO 以及乙酰乙酸酯和 3-氨基巴豆酸酯制备而成。 此外，还介绍了含有这些化合物的药物制剂。
• Amorphous lercanidipine hydrochloride and uses thereof
  申请人：Leonardi Amedeo

  公开号：US20060211742A1

  公开（公告）日：2006-09-21

  The invention provides a substantially pure amorphous lercanidipine hydrochloride having a purity of at least 95% pure, preferably at least about 97% pure, more preferably at least about 99% pure, and still more preferably at least about 99.5% pure. The invention further relates to methods of preparing substantially pure amorphous lercanidipine, as well as methods of providing rapid relief from hypertension by administering the substantially pure amorphous lercanidipine hydrochloride of the present invention to a patient in need of such treatment.

  本发明提供了一种纯度至少为 95%，优选纯度至少约为 97%，更优选纯度至少约为 99%，更优选纯度至少约为 99.5%的高纯度无定形盐酸氯卡尼平。本发明进一步涉及制备纯度相当高的无定形勒卡地平的方法，以及通过向需要治疗的患者施用本发明的纯度相当高的无定形盐酸勒卡地平来快速缓解高血压的方法。
• USE OF 1,4-DIHYDROPYRIDINE DERIVATIVES IN THE PREVENTION AND THERAPY OF ATHEROSCLEROTIC DEGRADATION OF ARTERIAL WALLS
  申请人：RECORDATI S.A. CHEMICAL and PHARMACEUTICAL COMPANY

  公开号：EP0839036B1

  公开（公告）日：1999-08-25