(2R,3S)-2-phenylpiperidin-3-amine | 1032169-90-6

• 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: (2R,3S)-2-phenylpiperidin-3-amine
• CAS: 1032169-90-6
• 化学式: C₁₁H₁₆N₂
• 分子量: 176.261
• InChiKey: GFMAFYNUQDLPBP-WDEREUQCSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  38
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (2R,3S)-2-phenylpiperidin-3-amine 、 邻甲氧基苯甲醛 在 三乙酰氧基硼氢化钠 作用下， 以 二氯甲烷 为溶剂， 反应 20.0h， 以70%的产率得到CP-99,994-1
  参考文献：
  名称：

  A Direct Stereoselective Approach to trans-2,3-Disubstituted Piperidines: Application in the Synthesis of 2-Epi-CP-99,994 and (+)-Epilupinine

  摘要：

  A simple synthesis of enantiomerically pure piperidine esters is described, offering a straightforward access to the trans-2,3-disubstituted piperidine skeleton which is present in a broad range of biologically active compounds.

  DOI：

  10.1021/ol800722a
• 作为产物：
  描述：

  benzyl (2R,3S)-2-phenyl-1-[(R)-1-phenylethyl]piperidin-3-ylcarbamate 在 盐酸 、 10% Pd on charcoal 、 氢气 作用下， 以 乙醇 、 水 为溶剂， 反应 12.0h， 以88%的产率得到(2R,3S)-2-phenylpiperidin-3-amine
  参考文献：
  名称：

  A Direct Stereoselective Approach to trans-2,3-Disubstituted Piperidines: Application in the Synthesis of 2-Epi-CP-99,994 and (+)-Epilupinine

  摘要：

  A simple synthesis of enantiomerically pure piperidine esters is described, offering a straightforward access to the trans-2,3-disubstituted piperidine skeleton which is present in a broad range of biologically active compounds.

  DOI：

  10.1021/ol800722a

文献信息

• 5-Phenylbenzylamine compounds, process for their production and intermediates for their synthesis
  申请人：——

  公开号：US20040097548A1

  公开（公告）日：2004-05-20

  The present invention relates to a 5-phenylbenzylamine compound represented by the formula [1]: 1 wherein Ring A represents a phenyl group having a substituent(s), R a , R b1 and R b2 each represent hydrogen atom, a halogen atom, a lower alkyl group, a halogeno-lower alkyl group or a lower alkoxy group, R c1 represents hydrogen atom, a lower alkyl group optionally substituted by a heterocyclic group, or an acyl group, R c2 and R e each represent hydrogen atom or a lower alkyl group, R d represents hydrogen atom, a lower alkyl group or an acyl group, and R f represents a lower alkyl group or a cyclic lower alkyl group, or a pharmaceutically acceptable salt thereof, a process for preparing the same and synthetic intermediate thereof.

  本发明涉及一种由公式（1）表示的5-苯基苄胺化合物：其中环A代表具有取代基（Ra，Rb1和Rb2）的苯基；Ra，Rb1和Rb2各代表氢原子、卤素原子、较低的烷基、卤代较低的烷基或较低的烷氧基；Rc1代表氢原子、可选地被杂环基取代的较低烷基或酰基；Rc2和Re各代表氢原子或较低的烷基；Rd代表氢原子、较低的烷基或酰基；Rf代表较低的烷基或环状较低的烷基，或其药学上可接受的盐，以及其制备方法和合成中间体。
• Process for the preparation of piperidinylaminomethyl trifluoromethyl cyclic ether compounds
  申请人：——

  公开号：US20030236268A1

  公开（公告）日：2003-12-25

  The present invention relates to a novel process for the preparation of a diastereomeric mixture of piperidinylaminomethyl trifluoromethyl cyclic ether compounds of formulae Ia and Ib: 1 and pharmaceutically acceptable salts thereof, wherein R 1 is C 1 -C 6 alkyl; R 2 is C 1 -C 6 alkyl, halo C 1 -C 6 alkyl or phenyl or substituted phenyl; R 3 is hydrogen or halo; m is zero, one or two, and wherein said mixture is highly enriched in the compound of formula Ia, and to novel processes for the preparation and purification of intermediate compounds useful in the preparation of compounds of formulae Ia and Ib.

  本发明涉及一种制备式Ia和Ib的哌啶基氨甲基三氟甲基环醚化合物的对映异构体混合物的新工艺及其药学上可接受的盐，其中R1是C1-C6烷基；R2是C1-C6烷基，卤代C1-C6烷基或苯基或取代苯基；R3是氢或卤素；m为零、一或二，所述混合物在式Ia的化合物中高度富集，并且本发明涉及一种用于制备式Ia和Ib化合物的中间体化合物的新工艺和纯化工艺。
• 5-PHENYLBENZYLAMINE COMPOUNDS, PROCESS FOR THEIR PRODUCTION AND INTERMEDIATES FOR THEIR SYNTHESIS
  申请人：TANABE SEIYAKU CO., LTD.

  公开号：EP1323713A1

  公开（公告）日：2003-07-02

  The present invention relates to a 5-phenylbenzylamine compound represented by the formula [1]: wherein Ring A represents a phenyl group having a substituent(s),    Ra, Rb1 and Rb2 each represent hydrogen atom, a halogen atom, a lower alkyl group, a halogeno-lower alkyl group or a lower alkoxy group,    Rc1 represents hydrogen atom, a lower alkyl group optionally substituted by a heterocyclic group, or an acyl group,    Rc2 and Re each represent hydrogen atom or a lower alkyl group,    Rd represents hydrogen atom, a lower alkyl group or an acyl group, and    Rf represents a lower alkyl group or a cyclic lower alkyl group, or a pharmaceutically acceptable salt thereof, a process for preparing the same and synthetic intermediate thereof.

  本发明涉及一种由式[1]表示的 5-苯基苄胺化合物： 其中环 A 代表具有取代基的苯基、 Ra、Rb1 和 Rb2 各自代表氢原子、卤素原子、低级烷基、卤素-低级烷基或低级烷氧基、 Rc1 代表氢原子、任选被杂环基取代的低级烷基或酰基、 Rc2 和 Re 分别代表氢原子或低级烷基、 Rd 代表氢原子、低级烷基或酰基，以及 Rf 代表低级烷基或环状低级烷基、 或其药学上可接受的盐、制备方法及其合成中间体。
• HETEROARYLAMINO AND HETEROARYLSULFONAMIDO SUBSTITUTED 3-BENZYLAMINOMETHYL PIPERIDINES AND RELATED COMPOUNDS
  申请人：PFIZER INC.

  公开号：EP0719266A1

  公开（公告）日：1996-07-03
• US6486325B1
  申请人：——

  公开号：US6486325B1

  公开（公告）日：2002-11-26