((1R,2R)-2-amino-cyclopentyl)-carbamic acid benzyl ester | 942492-53-7

• 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: ((1R,2R)-2-amino-cyclopentyl)-carbamic acid benzyl ester
• 英文别名: benzyl N-[(1R,2R)-2-aminocyclopentyl]carbamate
• CAS: 942492-53-7
• 化学式: C₁₃H₁₈N₂O₂
• 分子量: 234.298
• InChiKey: JUFLCFJTQMDCIG-VXGBXAGGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  64.4
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  氯甲酸苄酯 、 ((1R,2R)-2-amino-cyclopentyl)-carbamic acid benzyl ester 在 sodium carbonate 作用下， 以 水 为溶剂， 以91%的产率得到benzyl N-[(1R,2R)-2-(phenylmethoxycarbonylamino)cyclopentyl]carbamate
  参考文献：
  名称：

  Biocatalytic Approaches toward the Synthesis of Both Enantiomers of trans-Cyclopentane-1,2-diamine

  摘要：

  [GRAPHICS]A lipase-catalyzed double monoaminolysis of dimethyl malonate by (+/-)-trans-cyclopentane-1,2-diamine allows the sequential resolution of the latter compound, affording an enantiopure bis(amidoester), which is subsequently transformed into an optically active polyamine. As an alternative, both enantiomers of the diamine can be obtained from enantiopure (+)- or (-)-2-aminocyclopentanol, prepared by enzymatic resolution.

  DOI：

  10.1021/ol026574l
• 作为产物：
  描述：

  benzyl (1R,2S)-N-(2-hydroxycyclopentyl)carbamate 在 palladium on activated charcoal sodium azide 、 氢气 、 三乙胺 作用下， 以 甲醇 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 生成 ((1R,2R)-2-amino-cyclopentyl)-carbamic acid benzyl ester
  参考文献：
  名称：

  Biocatalytic Approaches toward the Synthesis of Both Enantiomers of trans-Cyclopentane-1,2-diamine

  摘要：

  [GRAPHICS]A lipase-catalyzed double monoaminolysis of dimethyl malonate by (+/-)-trans-cyclopentane-1,2-diamine allows the sequential resolution of the latter compound, affording an enantiopure bis(amidoester), which is subsequently transformed into an optically active polyamine. As an alternative, both enantiomers of the diamine can be obtained from enantiopure (+)- or (-)-2-aminocyclopentanol, prepared by enzymatic resolution.

  DOI：

  10.1021/ol026574l

文献信息

• PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH
  申请人：Bhattacharya Kumar Samit

  公开号：US20080234303A1

  公开（公告）日：2008-09-25

  The present invention relates to a compound of the formula 1 or a pharmaceutically acceptable salt thereof, wherein Ar is a group of formula and R 1 , R 2 , R 13 , A, K, M, L 1 , L 2 , X, Y 1 , Y 2 , Q, salt thereof, wherein R 1 , R 2 , R 13 , A, K, L 1 , L 2 , W, X, Z 1 , Z 2 , Y 1 , Y 2 , Z 1 , Z 2 , M, Q, W, X, m, p and q are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. The invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

  本发明涉及式1的化合物或其药学上可接受的盐，其中Ar是式的基团，而R1、R2、R13、A、K、M、L1、L2、X、Y1、Y2、Q、其盐、R1、R2、R13、A、K、L1、L2、W、X、Z1、Z2、Y1、Y2、Z1、Z2、M、Q、W、X、m、p和q的定义如本文所述。这些新型嘧啶衍生物在哺乳动物中治疗异常细胞增长，如癌症方面具有用途。本发明还涉及使用这些化合物在哺乳动物，特别是人类中治疗异常细胞增长的方法，以及含有这些化合物的制药组合物。
• ENZYMATIC SYNTHESIS OF ENANTIOMERICALLY ENRICHED DERIVATIVES OF CIS- AND TRANS-CYCLOPENTANE-1,2-DIAMINES
  申请人：EntreChem, S.L.

  公开号：EP2319825A1

  公开（公告）日：2011-05-11

  SUMMARY The present invention relates to the enzymatic resolution of cis-and trans-cyclopentane-1,2-diamine derivatives to obtain enantiomerically pure or enriched compounds, a method for the preparation of the starting materials of that procedure, the products of this procedure and its transformation into products of commercial interest.

  摘要 本发明涉及酶解顺式和反式环戊烷-1,2-二胺衍生物以获得对映体纯度或富集度高的化合物、制备该过程起始材料的方法、该过程的产物及其转化为具有商业价值的产品。
• US7820648B2
  申请人：——

  公开号：US7820648B2

  公开（公告）日：2010-10-26
• US8716314B2
  申请人：——

  公开号：US8716314B2

  公开（公告）日：2014-05-06
• [EN] PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH<br/>[FR] DÉRIVÉS PYRIMIDIQUES DESTINÉS À TRAITER UNE CROISSANCE CELLULAIRE ANORMALE
  申请人：PFIZER PROD INC

  公开号：WO2007072158A2

  公开（公告）日：2007-06-28

  (EN) The present invention relates to a compound of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein Ar is a group of Formula (II) and salts thereof. Such pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.(FR) La présente invention concerne un composé de formule (I) ou un sel pharmaceutiquement acceptable de ce dernier, formule dans laquelle Ar est un groupe de formule (III), et R1, R2, R13, A, K, M, L1, L2, X, Y1, Y2, Q, le sel dudit composé, R1, R2, R13, A, K, L1, L2, W, X, Z1, Z2, Y1, Y2, Z1, Z2, M, Q, W, X, m, p et q étant tels que définis. Ces nouveaux dérivés pyrimidiques sont utiles dans le traitement d'une croissance cellulaire anormale, telle que le cancer, chez des mammifères. Cette invention concerne également un procédé d'utilisation de ces composés dans le traitement d'une croissance cellulaire anormale chez des mammifères, en particulier des êtres humains, ainsi que des compositions pharmaceutiques contenant lesdits composés.