tert-Butyl (R)-3-amino-2,3-dihydrospiro[indene-1,4'-piperidine]-1'-carboxylate | 252008-75-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: tert-Butyl (R)-3-amino-2,3-dihydrospiro[indene-1,4'-piperidine]-1'-carboxylate
• 英文别名: tert-butyl (1R)-1-aminospiro[1,2-dihydroindene-3,4'-piperidine]-1'-carboxylate
• CAS: 252008-75-6
• 化学式: C₁₈H₂₆N₂O₂
• 分子量: 302.417
• InChiKey: MRMIQWNSSBRSLQ-OAHLLOKOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  55.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  tert-Butyl (R)-3-amino-2,3-dihydrospiro[indene-1,4'-piperidine]-1'-carboxylate 在 盐酸 、 三乙酰氧基硼氢化钠 、 三乙胺 作用下， 以 1,4-二氧六环 、 二氯甲烷 、 乙酸乙酯 为溶剂， 生成 3-[[(1R)-1-acetamidospiro[1,2-dihydroindene-3,4'-piperidine]-1'-yl]methyl]carbazole-9-carboxamide
  参考文献：
  名称：

  Discovery and characterization of a potent and selective antagonist of melanin-concentrating hormone receptor 2

  摘要：

  A series of spiropiperidine carbazoles were synthesized and evaluated as MCHR2 antagonists using a FLIPR assay. The pharmacokinetic properties of selected compounds have also been studied. This effort led to the discovery of potent and specific MCHR2 antagonists. Compound 38 demonstrated good pharmacokinetic properties across rat, beagle dog and rhesus monkey and had a favorable selectivity profile against a number of other receptors. These MCHR2 antagonists are considered appropriate tool compounds for study of the function of MCHR2 in vivo. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.10.125
• 作为产物：
  描述：

  2,3-二氢-3-氧代螺[1H-茚-1,4’-哌啶]-1’-甲酸叔丁酯 在 硼烷四氢呋喃络合物 、 叠氮磷酸二苯酯 、 水 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 、 三苯基膦 、 (S)-2-甲基-CBS-恶唑硼烷 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 生成 tert-Butyl (R)-3-amino-2,3-dihydrospiro[indene-1,4'-piperidine]-1'-carboxylate
  参考文献：
  名称：

  Discovery and characterization of a potent and selective antagonist of melanin-concentrating hormone receptor 2

  摘要：

  A series of spiropiperidine carbazoles were synthesized and evaluated as MCHR2 antagonists using a FLIPR assay. The pharmacokinetic properties of selected compounds have also been studied. This effort led to the discovery of potent and specific MCHR2 antagonists. Compound 38 demonstrated good pharmacokinetic properties across rat, beagle dog and rhesus monkey and had a favorable selectivity profile against a number of other receptors. These MCHR2 antagonists are considered appropriate tool compounds for study of the function of MCHR2 in vivo. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.10.125

文献信息

• Spiropiperidine derivatives as melanocortin receptor agonists
  申请人：——

  公开号：US20010029259A1

  公开（公告）日：2001-10-11

  Certain novel spiropiperidine compounds are agonists of melanocortin receptor(s) and are useful for the treatment, control or prevention of diseases and disorders responsive to the activation of melanocortin receptors. The compounds of the present invention are therefore useful for treatment of diseases and disorders such as obesity, diabetes, sexual dysfunction including erectile dysfunction and female sexual dysfunction.

  某些新型螺哌啶化合物是黑皮质素受体的激动剂，可用于治疗、控制或预防黑皮质素受体活化引起的疾病和紊乱。因此，本发明的化合物可用于治疗肥胖、糖尿病、性功能障碍（包括勃起功能障碍和女性性功能障碍）等疾病和紊乱。
• SPIROPIPERIDINE DERIVATIVES AS MELANOCORTIN RECEPTOR AGONISTS
  申请人：MERCK & CO., INC.

  公开号：EP1085869A1

  公开（公告）日：2001-03-28
• EP1085869A4
  申请人：——

  公开号：EP1085869A4

  公开（公告）日：2001-10-04
• US6294534B1
  申请人：——

  公开号：US6294534B1

  公开（公告）日：2001-09-25
• US6410548B2
  申请人：——

  公开号：US6410548B2

  公开（公告）日：2002-06-25