N-(tert-butoxycarbonyl)-4-propyl-piperidine-2-carboxylic acid | 941585-67-7

• 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: N-(tert-butoxycarbonyl)-4-propyl-piperidine-2-carboxylic acid
• 英文别名: 1-(Tert-butoxycarbonyl)-4-propylpiperidine-2-carboxylic acid；4-propyl-piperidine-1,2-dicarboxylic acid 1-tert-butyl ester；1-(tert-butoxycarbonyl)-4-propylpipecolic acid；N-Boc-4-propylpipecolinic acid；1-[(2-methylpropan-2-yl)oxycarbonyl]-4-propylpiperidine-2-carboxylic acid
• CAS: 941585-67-7
• 化学式: C₁₄H₂₅NO₄
• 分子量: 271.357
• InChiKey: DODVBDPZVCRICY-UHFFFAOYSA-N

物化性质

• 沸点：
  387.7±35.0 °C(Predicted)
• 密度：
  1.080±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  N-(tert-butoxycarbonyl)-4-propyl-piperidine-2-carboxylic acid 生成 4-Propyl-piperidine-2-carboxylic acid [(4-chloro-phenyl)-(3,4,5-trihydroxy-6-methylsulfanyl-tetrahydro-pyran-2-yl)-methyl]-amide
  参考文献：
  名称：

  Novel lincomycin derivatives possessing antibacterial activity

  摘要：

  新型的林可霉素衍生物已被披露。这些林可霉素衍生物表现出抗菌活性。本发明的化合物可能对细菌，包括革兰氏阳性生物，表现出强效活性，并可能是有用的抗微生物药剂。该化合物的合成和使用方法也已被披露。

  公开号：

  US20050215488A1
• 作为产物：
  描述：

  4-propyl-pyridine-2-carboxylic acid hydrochloride 在 platinum(IV) oxide sodium hydroxide 、 氢气 作用下， 以 水 、 叔丁醇 为溶剂， 20.0 ℃ 、101.33 kPa 条件下， 反应 48.0h， 生成 N-(tert-butoxycarbonyl)-4-propyl-piperidine-2-carboxylic acid
  参考文献：
  名称：

  EP1970377

  摘要：

  公开号：

文献信息

• Novel lincomycin derivatives possessing antimicrobial activity
  申请人：Lewis G. Jason

  公开号：US20050043248A1

  公开（公告）日：2005-02-24

  Novel lincomycin derivatives are disclosed. These lincomycin derivatives exhibit antibacterial activity. The compounds of the subject invention may exhibit potent activities against bacteria, including gram positive organisms, and may be useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.

  新型的林可霉素衍生物被披露。这些林可霉素衍生物表现出抗菌活性。本发明的化合物可能对细菌，包括革兰氏阳性生物，表现出强效活性，并且可能是有用的抗微生物药剂。该化合物的合成和使用方法也被披露。
• Synthesis and antibacterial activity of novel lincomycin derivatives. IV. Optimization of an N-6 substituent
  作者：Ko Kumura、Yoshinari Wakiyama、Kazutaka Ueda、Eijiro Umemura、Yoko Hirai、Keiko Yamada、Keiichi Ajito

  DOI：10.1038/ja.2017.143

  日期：2017.12

  pirlimycin and other related compounds. These dual modifications were accomplished by using methyl α-thiolincosaminide as a starting material. As a result of these dual modifications, the antibacterial activities were improved compared with those of compounds with a single modification at the C-7 position. The antibacterial activities of selected compounds in this report against macrolide-resistant

  描述了在C-6和C-7位置修饰的林可霉素衍生物的设计和合成。C-7位的取代基是5-芳基-1,3,4-噻二唑-2-基-硫基，该基团对带有erm基因的耐大环内酯性肺炎链球菌和化脓性链球菌产生抗菌活性。在应用有关Pirlimycin和其他相关化合物的信息时，还探索了C-6位的其他修饰。这些双重修饰是通过使用甲基α-硫代林糖胺作为起始原料来完成的。这些双重修饰的结果是，与在C-7位置具有单一修饰的化合物相比，抗菌活性得到了提高。本报告中所选化合物对大环内酯类耐药肺炎链球菌和肺炎链球菌的抗菌活性。
• LINCOSAMIDE DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT
  申请人：Umemura Eijirou

  公开号：US20100184746A1

  公开（公告）日：2010-07-22

  An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R 1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R 1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R 2 represents a hydrogen atom or C 1-6 alkyl; R 3 represents C 1-6 alkyl or C 3-6 cycloalkyl-C 1-4 alkyl; R 4 , R 5 , and R 6 represent a hydrogen atom; R 7 represents C 1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae . Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.

  本发明的目标是提供式（I）的化合物或其药理学上可接受的盐或溶剂，其中A代表芳基，而R1代表五元或六元单环杂环基，或A代表四至六元单环杂环基，而R1代表芳基或五元或六元单环杂环基；R2代表氢原子或C1-6烷基；R3代表C1-6烷基或C3-6环烷基-C1-4烷基；R4、R5和R6代表氢原子；R7代表C1-6烷基；m为1至3。这些化合物是新型的林可霉素衍生物，对耐药性肺炎链球菌具有强效活性。此外，这些化合物可用作抗微生物剂，对预防或治疗细菌感染性疾病有用。
• LINCOMYCIN DERIVATIVES AND ANTIMICROBIAL AGENTS COMPRISING THE SAME AS ACTIVE INGREDIENT
  申请人：Wakiyama Yoshinari

  公开号：US20100210570A1

  公开（公告）日：2010-08-19

  An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R 1 represents N-optionally substituted C 1-6 alkyl-N-optionally substituted C 1-6 alkylamino-C 1-6 alkyl; R 2 represents a hydrogen atom or optionally substituted C 1-6 alkyl; R 3 represents optionally substituted C 1-6 alkyl or C 3-6 cycloalkyl-C 1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.

  本发明的目标是提供以下化合物(1)或其药理学上可接受的盐或溶剂，其中A代表芳基；R1代表N-可选取代的C1-6烷基-N-可选取代的C1-6烷基氨基-C1-6烷基；R2代表氢原子或可选取代的C1-6烷基；R3代表可选取代的C1-6烷基或C3-6环烷基-C1-4烷基；m为1至3；n为0；p为0至2。这些化合物是新颖的林可霉素衍生物，对最近在感染性疾病治疗中引起问题的耐药性肺炎链球菌具有强效活性。此外，这些化合物可用作抗微生物药物，有助于预防或治疗细菌感染性疾病。
• Lincosamide derivatives and antimicrobial agents comprising the same as active ingredient
  申请人：Meiji Seika Kaisha, Ltd.

  公开号：US07867980B2

  公开（公告）日：2011-01-11

  An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or C1-6 alkyl; R3 represents C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; R4, R5, and R6 represent a hydrogen atom; R7 represents C1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.

  本发明的目标是提供式（I）的化合物或其药学上可接受的盐或溶剂，其中A代表芳基，而R1代表五元或六元单环杂环基，或A代表四元至六元单环杂环基，而R1代表芳基或五元或六元单环杂环基；R2代表氢原子或C1-6烷基；R3代表C1-6烷基或C3-6环烷基-C1-4烷基；R4、R5和R6代表氢原子；R7代表C1-6烷基；m为1至3。这些化合物是新型的林可霉素衍生物，对耐药性肺炎链球菌有强效活性。此外，这些化合物可用作抗微生物剂，并可用于预防或治疗细菌感染性疾病。