3-Hydroxy-1-(4-nitrobenzyloxycarbonyl)pyrrolidine | 85001-68-9

• 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: 3-Hydroxy-1-(4-nitrobenzyloxycarbonyl)pyrrolidine
• 英文别名: N-p-nitrobenzyloxycarbonyl-3-hydroxypyrrolidine；(3R)-3-hydroxy-1-(p-nitrobenzyloxycarbonyl)pyrrolidine；3-hydroxy-1-(p-nitrobenzyloxycarbonyl)pyrrolidine；(4-nitrophenyl)methyl 3-hydroxypyrrolidine-1-carboxylate
• CAS: 85001-68-9
• 化学式: C₁₂H₁₄N₂O₅
• 分子量: 266.254
• InChiKey: SDVOYYMETCCZLA-UHFFFAOYSA-N

物化性质

• 沸点：
  463.9±45.0 °C(Predicted)
• 密度：
  1.424±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  95.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  3-Hydroxy-1-(4-nitrobenzyloxycarbonyl)pyrrolidine 在 三氧化硫吡啶 、 三乙胺 作用下， 以 二甲基亚砜 为溶剂， 生成 1-(p-nitrobenzyloxycarbonyl)-3-pyrrolidinone
  参考文献：
  名称：

  EP1630162

  摘要：

  公开号：
• 作为产物：
  描述：

  3-羟基吡咯烷 、 氯甲酸对硝基苄酯 在 乙酸乙酯 、 magnesium sulfate 作用下， 以 dioxane-water 、 1,4-二氧六环 为溶剂， 反应 0.17h， 以3-hydroxy-1-(p-nitrobenzyloxycarbonyl)pyrrolidine (6.6 g) was obtained as a pale yellow solid的产率得到3-Hydroxy-1-(4-nitrobenzyloxycarbonyl)pyrrolidine
  参考文献：
  名称：

  2-Aminoquinoline derivatives

  摘要：

  本发明提供了由通式[I]表示的2-氨基喹啉衍生物[其中R1和R2代表低碳基、低环烷基等，或者R1和R2共同形成一个与它们结合的氮杂环的脂肪族氮杂环；R3、R4、R5、R6和R7代表氢、低碳基等；R8代表低碳基、低碳基氧杂基等；n代表0-4的整数]。这些化合物作为黑色素浓集激素受体拮抗剂，并且可用于治疗中枢神经系统疾病、心血管疾病和代谢性疾病。

  公开号：

  US20060287340A1

文献信息

• Novel carbapenem derivatives of quarternary salt type
  申请人：——

  公开号：US20030022881A1

  公开（公告）日：2003-01-30

  An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and &bgr;-lactamase-producing bacteria and are stable against DHP-1. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts thereof: 1 wherein R 1 represents H or methyl; R 2 and R 3 each independently represent H, halogen, lower alkyl or the like; R 4 represents optionally substituted lower alkylthio or the like; and R 5 represents optionally substituted lower alkyl or the like.

  本发明的目的在于提供对MRSA、PRSP、流感病毒和β-内酰胺酶产生菌具有强大抗生素活性的碳青霉烯衍生物，且对DHP-1稳定。根据本发明的化合物是由公式(I)表示的化合物或其药物可接受的盐：1其中R1代表H或甲基；R2和R3各自独立地代表H、卤素、低级烷基等；R4代表可选地取代的低级烷基亚磺酰基等；R5代表可选地取代的低级烷基等。
• Penem derivatives and antimicrobial agents containing the same
  申请人：SUNTORY LIMITED

  公开号：EP0774465A1

  公开（公告）日：1997-05-21

  Penem derivatives represented by the following Formula (I): wherein Z represents a hydroxyl group or a fluorine atom, R1 represents a substituted or unsubstituted alkyl, alkenyl, aralkyl group, aryl group, heterocyclic, or acyl group, or a hydrogen atom, and R2 represents a hydrogen atom or a carboxyl-protecting group; and pharmacologically acceptable salts thereof are antibacterial agents effective against, inter alia, methicillin-resistant Staphylococcus aureus. The derivatives and salts are novel except when R1 is ethyl and Z is hydroxyl. The analogous compounds in which R2 is a carboxyl-protecting group and any hydroxyl group represented by Z is protected are novel process intermediates.

  Penem衍生物由以下公式（I）表示：其中Z代表一个羟基团或氟原子，R1代表一个取代或未取代的烷基，烯基，芳基甲基，芳基，杂环基或酰基，或氢原子，R2代表一个氢原子或羧基保护基；及其药理学上可接受的盐是有效的抗菌剂，可用于治疗耐甲氧西林金黄色葡萄球菌等感染。这些衍生物和盐是新颖的，除非R1是乙基且Z是羟基。其中R2是羧基保护基且Z代表的任何羟基被保护的类似化合物是新颖的工艺中间体。
• Penem derivatives and antimicrobial agent containing the same
  申请人：Ishiguro Masaji

  公开号：US20050004092A1

  公开（公告）日：2005-01-06

  A penem derivative represented by the following formula (I): wherein R 1 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic thio group, a substituted or unsubstituted acylthio group, a mercapto group or a hydrogen atom, and R 2 represents a hydrogen atom or a carboxyl-protecting group; or a pharmacologically acceptable salt thereof. The compound (I) exhibits strong antibacterial activities, and especially, shows strong activities against MRSA. It is therefore useful not only as a general antibacterial agent but also as an antibacterial agent for MRSA against which no general antibacterial agents are recognized to be-effective.

  以下是公式（I）所代表的一种青霉烷衍生物： 其中，R1代表取代或未取代的烷基、取代或未取代的烯基、取代或未取代的芳基烷基、取代或未取代的芳基、取代或未取代的烷基硫基、取代或未取代的烯基硫基、取代或未取代的芳基烷基硫基、取代或未取代的芳基硫基、取代或未取代的杂环基、取代或未取代的杂环硫基、取代或未取代的酰基硫基、巯基或氢原子，R2代表氢原子或羧酸保护基；或其药学上可接受的盐。该化合物（I）表现出强大的抗菌活性，特别是对MRSA表现出强大的活性。因此，它不仅有用作一般抗菌剂，还有用作抗MRSA的抗菌剂，对于这种细菌，一般的抗菌剂被认为无效。
• 2-aminoquinoline derivatives
  申请人：Banyu Pharmaceutical Co., Ltd.

  公开号：US07485647B2

  公开（公告）日：2009-02-03

  This invention provides 2-aminoquinoline derivatives represented by a general formula [I] [in which R1 and R2 either stand for lower alkyl, lower cycloalkyl, etc., or R1 and R2 together form an aliphatic nitrogen-containing heterocycle with the nitrogen atom to which they bind; R3, R4, R5, R6 and R7 stand for hydrogen, lower alkyl, etc.; R8 stands for lower alkyl, lower alkyloxy, etc.; and n stands for an integer of 0-4]. The compounds act as melanin concentrating hormone receptor antagonist, and are useful as medicines for central nervous system disorders, cardiovascular disorders and metabolic disorders.

  本发明提供了由通式[I]表示的2-氨基喹啉衍生物 [其中R1和R2可以是低烷基、低环烷基等，或者R1和R2共同形成一个含氮的脂肪族杂环，其与它们结合的氮原子；R3、R4、R5、R6和R7代表氢、低烷基等；R8代表低烷基、低烷氧基等；n代表0-4的整数]。这些化合物作为黑色素浓集激素受体拮抗剂，可用于中枢神经系统疾病、心血管疾病和代谢性疾病的药物。
• NOVEL CARBAPENEM DERIVATIVES OF QUATERNARY SALT TYPE
  申请人：Meiji Seika Kaisha, Ltd.

  公开号：EP1251134A1

  公开（公告）日：2002-10-23

  An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and β-lactamase-producing bacteria and are stable against DHP-1. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts thereof: wherein R1 represents H or methyl; R2 and R3 each independently represent H, halogen, lower alkyl or the like; R4 represents optionally substituted lower alkylthio or the like; and R5 represents optionally substituted lower alkyl or the like.

  本发明的目的是提供碳青霉烯类衍生物，它们对 MRSA、PRSP、流感病毒和产 β-内酰胺酶细菌具有强效抗生素活性，并且对 DHP-1 稳定。根据本发明的化合物是由式（I）代表的化合物或其药学上可接受的盐： 其中 R1 代表 H 或甲基；R2 和 R3 各自独立地代表 H、卤素、低级烷基或类似物；R4 代表任选取代的低级烷硫基或类似物；R5 代表任选取代的低级烷基或类似物。