(S)-1,5-dimethyl-2-piperidone

• 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: (S)-1,5-dimethyl-2-piperidone
• 英文别名: (5S)-1,5-dimethylpiperidin-2-one
• 化学式: C₇H₁₃NO
• 分子量: 127.186
• InChiKey: YXHVIDNQBMVYHQ-LURJTMIESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.86
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  2-溴-5-甲基吡啶 在 [bis(2-methylallyl)cycloocta-1,5-diene]ruthenium(II) 、 1,3-bis-(1(R)-phenyl-ethyl)-4,5-dihydro-3H-imidazol-1-ium tetrafluoroborate 、 potassium tert-butylate 、 氢气 作用下， 以 1,4-二氧六环 、 2-甲基-2-丁醇 、 正己烷 为溶剂， -10.0~100.0 ℃ 、12.0 MPa 条件下， 反应 106.0h， 生成 (S)-1,5-dimethyl-2-piperidone 、 (R)-1,5-dimethyl-2-piperidone
  参考文献：
  名称：

  Asymmetric Homogeneous Hydrogenation of 2-Pyridones

  摘要：

  An asymmetric homogeneous hydrogenation of 2(1H)-pyridones has been developed, using a ruthenium complex bearing two chiral N-heterocyclic carbene (NHC) ligands. To the best of our knowledge, the presented reaction is the first example of a homogeneous asymmetric conversion of 2-pyridones into the corresponding enantioenriched 2-piperidones.

  DOI：

  10.1055/s-0034-1378703

文献信息

• HETEROCYCLE-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES
  申请人：Pouzet Pascale

  公开号：US20100305102A1

  公开（公告）日：2010-12-02

  The invention relates to new dihydrothienopyrimidinesulphoxides of formula 1, as well as pharmacologically acceptable salts thereof, wherein X is SO or SO 2 , but preferably SO, and wherein R 3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl and wherein R 1 and R 2 have the meanings stated in claim 1, as well as pharmaceutical compositions which contain these compounds. These new dihydrothienopyrimidinesulphoxides are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers.

  该发明涉及公式1的新二氢噻吡嘧啶磺氧化物，以及其药理学上可接受的盐，其中X为SO或SO2，但最好为SO，其中R3表示一个可选择取代的、单环或双环的、不饱和的、部分饱和的或饱和的杂环，或一个可选择取代的、单环或双环的杂芳基，其中R1和R2具有权利要求1中所述的含义，以及含有这些化合物的药物组合物。这些新的二氢噻吡嘧啶磺氧化物适用于治疗呼吸道或胃肠道疾病，关节、皮肤或眼睛的炎症性疾病，外周或中枢神经系统疾病或癌症。
• NOVEL PHENYL-SUBSTITUTED PIPERAZINO-DIHYDROTHIENOPYRIMIDINES
  申请人：Pouzet Pascale

  公开号：US20110028441A1

  公开（公告）日：2011-02-03

  The invention relates to novel dihydrothienopyrimidines of the formula 1, and to pharmacologically acceptable salts thereof, formula (1) in which X is SO or SO 2 , but preferably SO, and either R 3 is a monosubstituted phenyl ring in the ortho position or in the meta position, or R 3 is a phenyl ring bisubstituted in any positions, and pharmaceutical compositions which comprise these compounds. These novel dihydrothienopyrimidines are suitable for the treatment of respiratory or gastrointestinal symptoms or disorders, inflammatory disorders of the joints, of the skin or of the eyes, disorders of the peripheral or central nervous system or cancers.

  该发明涉及公式1的新型二氢噻吡嘧啶化合物，以及其药学上可接受的盐，公式（1）中X为SO或SO2，但最好为SO，R3为邻位或间位单取代苯环，或R3为苯环多取代的任意位置，并包含这些化合物的药物组合物。这些新型二氢噻吡嘧啶化合物适用于治疗呼吸道或消化道症状或疾病、关节炎炎症性疾病、皮肤或眼部炎症性疾病、外周或中枢神经系统疾病或癌症。
• DRUG COMBINATIONS CONTAINING PDE4 INHIBITORS AND NSAIDS
  申请人：NICKOLAUS Peter

  公开号：US20120028932A1

  公开（公告）日：2012-02-02

  The present invention relates to new drug combinations which contain in addition to one or more PDE4-inhibitors at least one NSAID (=non-steroidal anti-inflammatory drug) (2), processes for preparing them and their use in treating in particular respiratory complaints such as for example COPD, chronic sinusitis and asthma. The invention particularly relates to those drug combinations which, in addition to one or more, preferably one PDE4 inhibitor of general formula 1 wherein X is SO or SO 2 , but preferably SO, and wherein R 3 denotes an optionally substituted, mono- or bicyclic, unsaturated, partly saturated or saturated heterocyclic group or an optionally substituted, mono- or bicyclic heteroaryl and wherein R 1 and R 2 have the meanings given in claim 1, contain at least one NSAID (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.

  本发明涉及包含除一个或多个PDE4抑制剂外，至少一个NSAID（非甾体抗炎药）的新药物组合，以及用于制备它们的方法以及它们在治疗呼吸道疾病（如COPD、慢性鼻窦炎和哮喘等）中的用途。该发明特别涉及那些药物组合，除了一个或多个，最好是一个一般式1中X为SO或SO2，但最好是SO，且其中R3表示一个可选择取代的、单环或双环、不饱和、部分饱和或饱和的杂环基团或一个可选择取代的、单环或双环杂芳基，其中R1和R2具有权利要求1中给出的含义，至少包含一个NSAID（2），其制备和用于治疗呼吸道疾病。
• PIPERAZINO-DIHYDROTHIENOPYRIMIDINE DERIVATIVES
  申请人：POUZET Pascale

  公开号：US20130274264A1

  公开（公告）日：2013-10-17

  A method for treating diseases associated with the inhibition of phosphodiesterase 4 (PDE4) enzyme in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a dihydrothienopyrimidinesulphoxide of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof

  一种治疗与磷酸二酯酶4（PDE4）酶抑制相关的疾病的方法，包括向需要治疗的患者投予公式1的二氢噻唑嘧啶硫氧化物的治疗有效量，以及其药理学上可接受的盐，对映异构体，对映体，外消旋体，水合物或溶剂化物。
• [EN] MALT-1 MODULATORS<br/>[FR] MODULATEURS DE MALT-1
  申请人：EXSCIENTIA LTD

  公开号：WO2022106857A1

  公开（公告）日：2022-05-27

  Disclosed are compounds, compositions and methods for treating disease, syndromes, conditions and disorders that are affected by the modulation of MALT-1. Such compounds are represented by Formula (I) and Formula (II), wherein the variables are defined herein.

  本发明涉及通过调节MALT-1影响的治疗疾病、综合症、病况和疾患的化合物、组合物和方法。这些化合物由公式（I）和公式（II）所表示，其中变量在此定义。