L(+)-α-Propylamino-2-methyl-propioanilid | 14289-31-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: L(+)-α-Propylamino-2-methyl-propioanilid
• 英文别名: (+)-Prilocaine；(S)-N-(2-Methylphenyl)-2-(propylamino)propanamide；(2S)-N-(2-methylphenyl)-2-(propylamino)propanamide
• CAS: 14289-31-7
• 化学式: C₁₃H₂₀N₂O
• 分子量: 220.315
• InChiKey: MVFGUOIZUNYYSO-NSHDSACASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  16
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  41.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  丙胺卡因 生成 L(+)-α-Propylamino-2-methyl-propioanilid
  参考文献：
  名称：

  Tegner,C.; Willman,N.-E., Acta Chemica Scandinavica (1947), 1961, vol. 15, p. 1180 - 1181

  摘要：

  DOI：

文献信息

• Chiral Discrimination of Acyclic Secondary Amines by ¹⁹F NMR
  作者：Guangxing Gu、Chong Zhao、Wei Zhang、Jiajin Weng、Zhenchuang Xu、Jian Wu、Yingbo Xie、Xiao He、Yanchuan Zhao

  DOI：10.1021/acs.analchem.3c03846

  日期：2024.1.16

  Chiral aliphatic amine compounds exhibit a range of physiological activities, making them highly sought-after in the pharmaceutical industry and biological research. One notable obstacle in studying these compounds stems from the pronounced steric hindrance surrounding the nitrogen atom. This characteristic often leads to a weak affinity of acyclic secondary amines for molecular probes, making their

  手性脂肪胺化合物表现出一系列的生理活性，使其在制药工业和生物研究中备受追捧。研究这些化合物的一个显着障碍源于氮原子周围明显的空间位阻。这一特性通常导致无环仲胺对分子探针的亲和力较弱，使得它们的手性辨别变得复杂。为了应对这一挑战，我们的研究推出了一种新型19 F 标记探针，能够识别和区分这些无环仲胺的对映体。通过策略性地合并单个氟原子作为19 F 标记，我们成功地减少了结合位点的空间位阻。这种改变增强了探针对体积较大的分析物的亲和力。为了证明其有效性，我们已成功地将我们的探针用于相关药物的手性分析，准确地确定了它们的对映体组成。
• Local anesthetic mixture for topical application, and process for its preparation
  申请人：Astra Läkemedel Aktiebolag

  公开号：EP0002425A1

  公开（公告）日：1979-06-13

  The present invention relates to pharmacological active preparations, especialiy local anesthetic preparations and deals with the problem of obtaining a solution of a local anesthetic agent in the form of its base, where the concentration is higher than otherwise possible. This problem has been dissolved according to the present invention thereby that one local anesthetic agent in the form of its base and as such having a melting point of 30 to 50 C, preferably prilocaine or tetracaine, is provided with one other local anesthitic agent in the form of its base and as such having a melting point of above 30 C, preferably above 40 C, preferably benzocaine. lidocaine, bupivacaine, mepivacaine, etidocaine or tetracaine which agents when brought and heated together form a homogenous oil having a melting temperature of preferably below 40, more preferably below 25 C.

  本发明涉及药理活性制剂，特别是局部麻醉制剂，并解决了以基质形式获得局部麻醉剂溶液的问题，在这种溶液中，局部麻醉剂的浓度高于其他可能的浓度。本发明解决了这一问题，即在一种熔点为 30 至 50 摄氏度的基质局麻药（最好是普鲁卡因或四卡因）中加入另一种熔点高于 30 摄氏度（最好高于 40 摄氏度）的基质局麻药（最好是苯佐卡因）。这些药剂在一起加热时会形成熔点低于 40 摄氏度，更低于 25 摄氏度的均质油。
• Antiperspirant
  申请人：Playtex-Wallco Aktiebolag

  公开号：EP0002426A1

  公开（公告）日：1979-06-13

  The present invention relates to antiperspirants which shall have a rapid onset in order to obtain an immediate inhibition of perspiration. The invention thereby relates to antiperspirants which comprise a local anesthetic agent, whereby the invention is characterized in that the antiperspirant comprises a local anesthetic agent of the group prilocaine, bensocaine, lidocaine, bupivacaine, mepivacaine, etidocaine, ketocaine, 2-(2-n-butyloxyphenoxy)-1-diisopropylaminoethane, tetracaine, butanilicaine, trimecaine, dibucaine, quinisocaine, butacaine, oxybuprocaine and toylcaine. Preferred compositions comprises a mixture of prilocaine, tetracaine, butanilicaine, and trimecaine in the form of its base and one of the compounds bensocaine, lidocaine, bupivacaine, mepivacaine, dibucaine, and etidocaine, as well as tetracaine, butanilicaine and trimecaine. The antiperspirant is to be used elsewhere on a body where excessive perspiration occurs, preferably in axillae and on the hands.

  本发明涉及的止汗剂起效迅速，可立即抑制出汗。因此，本发明涉及一种含有局部麻醉剂的止汗剂，其特征在于该止汗剂含有一种局部麻醉剂，该局部麻醉剂属于prilocaine, bensocaine, lidocaine, bupivacaine, mepivacaine、bensocaine、lidocaine、bupivacaine、mepivacaine、etidocaine、ketocaine、2-(2-n-butyloxyphenoxy)-1-diisopropylaminoethane、tetracaine、butanilicaine、trimecaine、dibucaine、quinisocaine、butacaine、oxybuprocaine 和 toylcaine。优选的成分包括普鲁卡因、四卡因、丁胺卡因和三甲卡因的混合物，以其基质的形式和苯佐卡因、利多卡因、布比卡因、甲哌卡因、地布卡因和依替卡因以及四卡因、丁胺卡因和三甲卡因中的一种化合物。止汗剂可用于身体其他出汗过多的部位，最好是腋窝和手部。
• THERAPEUTIC CAUSING CONTRACTION OF MUCOSAL TISSUE, METHOD OF TREATING DISEASES RELATING TO MUCOSAL TISSUES, INJECTOR AND THERAPEUTIC SET
  申请人：Japan Science and Technology Agency

  公开号：EP1557163A1

  公开（公告）日：2005-07-27

  It is intended to provide a therapeutic causing contraction of a mucosal tissue whereby various diseases relating to mucosal tissues can be easily, safely and little invasively treated, a method of treating various diseases relating to mucosal tissues with the use of the therapeutic causing contraction of a mucosal tissue, and an injector and a therapeutic set usable in the treatment method. Namely, a therapeutic causing contraction of nasal mucosal tissue containing ethanol as the active ingredient preferably together with a steroid and/or an antihistaminic agent; a method of treating diseases with mucosal inflammation using the above therapeutic causing contraction of a mucosal tissue, and an injector and a therapeutic set usable in the treatment method.

  本发明的目的是提供一种可使粘膜组织收缩的治疗剂，从而可方便、安全和微创地治疗与粘膜组织有关的各种疾病；一种使用可使粘膜组织收缩的治疗剂治疗与粘膜组织有关的各种疾病的方法；以及一种可用于该治疗方法的注射器和治疗套装。即，一种可引起鼻粘膜组织收缩的治疗剂，其有效成分最好含有乙醇和类固醇及/或抗组胺剂；一种使用上述可引起粘膜组织收缩的治疗剂治疗粘膜炎症疾病的方法，以及一种注射器和一套可用于该治疗方法的治疗设备。
• Methods and systems of delivering medication via inhalation
  申请人：Next Safety, Inc.

  公开号：EP1911481A2

  公开（公告）日：2008-04-16

  Systems and methods for delivery of a drug to the respiratory system of a patient where the drug is supplied at a positive pressure relative to atmospheric pressure are provided. In particular, the drugs are delivered to the respiratory system of a patient who is capable of unassisted breathing. With the systems and methods of the present disclosure, medication available in a variety of forms is introduced in a controlled fashion into the air stream in aerosol, nebulized, or vaporized form.

  提供了向病人的呼吸系统输送药物的系统和方法，其中药物是在相对于大气压的正压下提供的。特别是，将药物输送到能够进行无助呼吸的患者的呼吸系统。利用本公开的系统和方法，可将各种形式的药物以气溶胶、雾化或汽化的形式有控制地引入气流中。