1-(氯乙酰基)-(9ci)-2-吡咯烷酮 | 43170-60-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: 1-(氯乙酰基)-(9ci)-2-吡咯烷酮
• 英文名称: 1-(2-chloro-acetyl)-pyrrolidin-2-one
• 英文别名: PCM-0102982；N-chloroacetyl-2-pyrrolidinone；N-(2-chloroacetyl)-pyrrolidin-2-one；N-(chloroacetyl)pyrrolidone；1-(2-chloroacetyl)pyrrolidin-2-one
• CAS: 43170-60-1
• 化学式: C₆H₈ClNO₂
• mdl: MFCD03973204
• 分子量: 161.588
• InChiKey: XAXRVMNVJFVLDQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.666
• 拓扑面积：
  37.4
• 氢给体数：
  0
• 氢受体数：
  2

安全信息

• 危险等级：
  IRRITANT
• 海关编码：
  2933790090

反应信息

• 作为反应物：
  描述：

  1-(氯乙酰基)-(9ci)-2-吡咯烷酮 在 palladium on activated charcoal 盐酸 、 sodium azide 、 氢气 作用下， 以 甲醇 、 水 、 丙酮 为溶剂， 反应 5.5h， 生成 N-(2-aminoacetyl)-2-pyrrolidone
  参考文献：
  名称：

  Angulo, Larry; Nunez, Oswaldo, Journal of Chemical Research, Miniprint, 1996, # 5, p. 1123 - 1146

  摘要：

  DOI：
• 作为产物：
  描述：

  2-吡咯烷酮 、 氯乙酰氯 以 甲苯 为溶剂， 反应 6.0h， 以to give 74.5 g of N-(chloroacetyl)pyrrolidone的产率得到1-(氯乙酰基)-(9ci)-2-吡咯烷酮
  参考文献：
  名称：

  Quaternary ammonium compounds as bleach activators and their preparation

  摘要：

  四价铵化合物，其制备和用途。公式I的化合物 ##STR1## 被认为是新颖的，其中基团R.sub.1、R.sub.2和R.sub.3是有机取代基，L是内酰胺或环状胺，X是适当的阴离子。这些新颖的化合物被用作清洁剂和具有漂白作用的洗涤剂中的漂白活化剂。

  公开号：

  US05952283A1

文献信息

• Novel compounds for the management of aging-related and diabetic vascular complications, process for their preparation, therapeutic and cosmetic uses thereof
  申请人：TORRENT PHARMACEUTICALS LTD.

  公开号：US20030045554A1

  公开（公告）日：2003-03-06

  The invention discloses a new clause of a five membered heterocylic ring compounds of general formula 1 1 and its pharmaceutically or cosmetically acceptable salts, wherein R1, R2, R3, R4, R5, A, B, X and Y are as defined in the specification. The invention also discloses a process for preparation of these compound and their therapeutic and cosmetic applications particularly in the management of aging related and diabetic vascular complications. The compounds in question act by triple action of an AGE (Advanced Glycation Endproducts) breaker, AGE inhibitor and free radical scavenger which make them most suitable in different therapeutic and cosmetic applications. The invention also discloses pharmaceuticals and cosmetic compositions comprising these compounds and method of treatment of diseases caused by accumulation of AGE and/or free radicals in the body cells.

  本发明公开了一种新的通式11的五元杂环化合物及其药学或美容学可接受的盐，其中R1、R2、R3、R4、R5、A、B、X和Y在说明书中定义。本发明还公开了制备这些化合物及其治疗和美容应用的方法，特别是在管理与衰老相关和糖尿病血管并发症方面。所述化合物通过AGE（高级糖基化终产物）断裂剂、AGE抑制剂和自由基清除剂的三重作用发挥作用，使它们在不同的治疗和美容应用中最为适用。本发明还公开了包含这些化合物的药物和化妆品组合物以及治疗由体细胞中AGE和/或自由基积累引起的疾病的方法。
• QUINOLINE-CARBOXAMIDE DERIVATIVES AS P2Y12 ANTAGONISTS
  申请人：Nazaré Marc

  公开号：US20100135999A1

  公开（公告）日：2010-06-03

  The present invention relates to compounds of the formula I, in which R 1 ; R 2 ; R 3 ; R 4 ; R 5 ; R 6 ; Z; A; B; E; X; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

  本发明涉及公式I的化合物，其中R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; V; G和M具有所述声明中指示的含义。公式I的化合物是有价值的药理活性化合物。它们对血小板具有强烈的抗聚集作用，从而具有抗血栓作用，适用于治疗和预防心血管疾病，如血栓栓塞病或再狭窄。它们是血小板ADP受体P2Y12的可逆拮抗剂，通常适用于存在不良激活血小板ADP受体P2Y12的情况，或者治愈或预防需要抑制血小板ADP受体P2Y12的情况。此外，本发明还涉及制备公式I化合物的方法，它们的用途，特别是作为药物中的活性成分，以及包含它们的制药制剂。
• Quinoline-carboxamide derivatives as P2Y12 antagonists
  申请人：Nazare Marc

  公开号：US08669266B2

  公开（公告）日：2014-03-11

  The present invention relates to compounds of the formula I, in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

  本发明涉及公式I的化合物，其中R1; R2; R3; R4; R5; R6; Z; A; B; E; X; Q; J; V; G和M具有所述权利要求中指定的含义。公式I的化合物是有价值的药理活性化合物。它们在血小板上表现出强烈的抗聚集作用，因此具有抗血栓作用，适用于治疗和预防心血管疾病，如血栓栓塞病或再狭窄。它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可以应用于存在不希望的血小板ADP受体P2Y12激活或需要抑制血小板ADP受体P2Y12的治疗或预防的情况。此外，本发明还涉及公式I的化合物的制备方法，它们的使用，特别是作为药物的活性成分，以及包含它们的药物制剂。
• HETEROCYCLIC PYRAZOLE-CARBOXAMIDESAS P2Y12 ANTAGONISTS
  申请人：Nazaré Marc

  公开号：US20110021537A1

  公开（公告）日：2011-01-27

  The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

  本发明涉及式I的化合物，其中R1；R2；Z；A；B；D；Q；J；V；G和M具有所述声明中指示的含义。式I的化合物是有价值的药理活性化合物。它们对血小板具有强烈的抗聚集作用，因此具有抗血栓作用，适用于治疗和预防心血管疾病，如血栓栓塞性疾病或再狭窄。它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常适用于存在不希望的血小板ADP受体P2Y12激活的情况，或者用于治疗或预防需要抑制血小板ADP受体P2Y12的情况。此外，本发明还涉及式I化合物的制备方法，它们的用途，特别是作为药物中的活性成分，以及包含它们的制剂。
• Novel compounds for the management of aging-related and diabetic vascular complications, process for their preparation and therapeutic uses thereof
  申请人：——

  公开号：US20010018524A1

  公开（公告）日：2001-08-30

  Novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof, 1 wherein, R 1 , R 2 , R 3 , X and m are as defined in the specification. Also disclosed is a method for preparation of the compounds of general formula (I) and pharmaceutical composition containing one or more compounds as defined above as active ingredients. Also disclosed is a method of treatment of a diabetic patient by administering the compounds as defined above, either singly or in combination with drugs for antidiabetic therapy.

  本发明涉及一系列新的吡啶系列化合物，可用于管理糖尿病和与衰老相关的血管并发症，包括肾脏疾病、神经损伤、动脉硬化、视网膜病变、皮肤疾病和牙齿变色，通过破坏预先形成的AGE，其通式为I，或其药学上可接受的盐，其中，R1、R2、R3、X和m如规范中所定义。本发明还公开了一种制备通式（I）化合物的方法和含有一种或多种上述化合物作为活性成分的制药组合物。本发明还公开了一种通过单独或与抗糖尿病治疗药物联合使用上述化合物治疗糖尿病患者的方法。