N-t-butyloxycarbonyl-3-methoxymethyloxy-4-hydroxymethylpiperidine | 217808-07-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: N-t-butyloxycarbonyl-3-methoxymethyloxy-4-hydroxymethylpiperidine
• 英文别名: Tert-butyl 4-(hydroxymethyl)-3-(methoxymethoxy)piperidine-1-carboxylate
• CAS: 217808-07-6
• 化学式: C₁₃H₂₅NO₅
• 分子量: 275.345
• InChiKey: JGNBOQGZESBKFH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  19
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.92
• 拓扑面积：
  68.2
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N-t-butyloxycarbonyl-3-methoxymethyloxy-4-hydroxymethylpiperidine 在 pyridinium chlorochromate 作用下， 生成 N-t-butyloxycarbonyl-3-methoxymethyloxy-4-(1-hydroxypropargyl)piperidine
  参考文献：
  名称：

  Ueda; Irie; Fukushi, Journal of labelled compounds and radiopharmaceuticals, 1999, vol. 42, # SUPPL. 1, p. S762-S764

  摘要：

  DOI：
• 作为产物：
  描述：

  3-氧代-4-哌啶甲酸乙酯 在 sodium tetrahydroborate 、 锂硼氢 作用下， 生成 N-t-butyloxycarbonyl-3-methoxymethyloxy-4-hydroxymethylpiperidine
  参考文献：
  名称：

  Ueda; Irie; Fukushi, Journal of labelled compounds and radiopharmaceuticals, 1999, vol. 42, # SUPPL. 1, p. S762-S764

  摘要：

  DOI：

文献信息

• [EN] PHENYL-HETEROARYL DERIVATIVES AND METHODS OF USE THEREOF<br/>[FR] DÉRIVÉS DE PHÉNYL-HÉTÉROARYLE ET PROCÉDÉS D'UTILISATION DE CEUX-CI
  申请人：TRANSTECH PHARMA INC

  公开号：WO2011103091A1

  公开（公告）日：2011-08-25

  The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.

  本发明提供了式（I）的苯基-杂环芳基衍生物及其药学上可接受的盐。这些化合物在治疗RAGE介导的疾病，如阿尔茨海默病方面是有用的。本发明还涉及制备式（I）化合物及其药学上可接受的盐的方法，包括含有这些化合物的药物组合物，以及在治疗RAGE介导的疾病中使用这些化合物和/或药物组合物的用途。
• Reagents for assaying central local acetylcholinesterase activity
  申请人：Daiichi Pure Chemicals Co., Ltd.

  公开号：US06306882B1

  公开（公告）日：2001-10-23

  The present invention relates to N-alkylpiperidine derivatives represented by general formula (1) or (2); wherein R1 represents optionally fluorinated lower alkyl; R2 represents lower alkyl; and R3 represents alkenyl substituted at the 1-position with hydroxy, lower alkoxy, lower alkoxyalkyloxy, lower alkoxyalkyloxyalkyloxy, or lower alkanoyloxy and substituted at the end with radioactive iodine, or alkenyloxymethyl substituted at the end with a radioactive iodine reagent containing the same for assaying central local AchE activity; a method for assaying the central local AchE activity; and labeled precursors of the above compounds. After easily passing through the blood-brain barrier, these compounds are hydrolyzed specifically by AchE in the brain into alcohols, which are then captured by the brain. In contrast, alcohols formed outside the brain do not migrate into the brain. The compounds of the invention emit &ggr;-rays at an appropriate energy level. These characteristics make the compounds highly useful as tracers for SPECT in assaying the central AchE activity.

  本发明涉及一种由通式（1）或（2）表示的N-烷基哌啶衍生物；其中R1代表可选择氟化的较低烷基；R2代表较低烷基；R3代表在1位被羟基、较低烷氧基、较低烷氧基烷氧基、较低烷氧基烷氧基烷氧基或较低烷酰氧基取代的烯基，并在末端被放射性碘取代，或在末端被含有放射性碘试剂的烯氧甲基取代，用于检测中枢局部AchE活性；一种检测中枢局部AchE活性的方法；以及上述化合物的标记前体。这些化合物容易穿过血脑屏障，然后在大脑中被AchE特异性水解成醇，然后被大脑捕获。相比之下，在大脑外形成的醇不会迁移到大脑。本发明的化合物在适当能级发射γ射线。这些特性使得这些化合物在检测中枢AchE活性的SPECT示踪剂中非常有用。
• Reagents for the determination of cerebral regional acetylcholinesterase activity
  申请人：DAIICHI PURE CHEMICALS CO., LTD

  公开号：US20020127180A1

  公开（公告）日：2002-09-12

  The present invention relates to N-alkylpiperidine derivatives represented by general formula (1) or (2); 1 wherein R 1 represents optionally fluorinated lower alkyl; R 2 represents lower alkyl; and R 3 represents alkenyl substituted at the 1-position with hydroxy, lower alkoxy, lower alkoxyalkyloxy, lower alkoxyalkyloxyalkyloxy, or lower alkanoyloxy and substituted at the end with radioactive iodine, or alkenyloxymethyl substituted at the end with a radioactive iodine reagent containing the same for assaying central local AchE activity; a method for assaying the central local AchE activity; and labeled precursors of the above compounds. After easily passing through the blood-brain barrier, these compounds are hydrolyzed specifically by AchE in the brain into alcohols, which are then captured by the brain. In contrast, alcohols formed outside the brain do not migrate into the brain. The compounds of the invention emit &ggr;-rays at an appropriate energy level. These characteristics make the compounds highly useful as tracers for SPECT in assaying the central AchE activity.

  本发明涉及由通式（1）或（2）表示的N-烷基哌啶衍生物；其中R1表示可选的氟化较低烷基；R2表示较低烷基；R3表示在1位被羟基，较低烷氧基，较低烷氧烷氧基，较低烷氧烷氧烷氧烷基或较低烷酰氧基取代的烯基，并在末端用放射性碘取代，或在末端用含有放射性碘试剂的烯氧甲基取代，用于测定中央局部AchE活性的方法；以及上述化合物的标记前体。这些化合物易于通过血脑屏障，特异性地被脑内AchE水解成醇，然后被大脑捕获。相比之下，在大脑外形成的醇不会迁移到大脑中。本发明的化合物以适当的能量水平发射γ射线，这些特性使得这些化合物在测定中央AchE活性的SPECT示踪剂中非常有用。
• PHENYL-HETEROARYL DERIVATIVES AND METHODS OF USE THEREOF
  申请人：Gohimukkula Devi R.

  公开号：US20110230458A1

  公开（公告）日：2011-09-22

  The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.

  本发明提供了式（I）的苯基-杂环取代衍生物及其药学上可接受的盐。这些化合物在治疗RAGE介导的疾病，如阿尔茨海默病中是有用的。本发明还涉及制备式（I）化合物及其药学上可接受的盐的方法，包括这些化合物的制药组合物，以及在治疗RAGE介导的疾病时使用这些化合物和/或制药组合物。
• Phenyl-Heteroaryl Derivatives and Methods of Use Thereof
  申请人：TransTech Pharma, Inc.

  公开号：US20130197007A1

  公开（公告）日：2013-08-01

  The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.

  本发明提供了式（I）的苯基-杂环芳基衍生物及其药学上可接受的盐。这些化合物可用于治疗RAGE介导的疾病，如阿尔茨海默病。本发明还涉及制备式（I）的化合物及其药学上可接受的盐的方法，包括这种化合物的制药组合物，以及使用这种化合物和/或制药组合物治疗RAGE介导的疾病。