(R)-1'-methyl-[1,3']bipyrrolidine | 1246300-48-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: (R)-1'-methyl-[1,3']bipyrrolidine
• 英文别名: (3R)-1-methyl-3-pyrrolidin-1-ylpyrrolidine
• CAS: 1246300-48-0
• 化学式: C₉H₁₈N₂
• 分子量: 154.255
• InChiKey: NFLOMKBBJCRGIP-SECBINFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  6.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  tert-butyl (R)-[1,3'-bipyrrolidine]-1'-carboxylate 在 lithium aluminium tetrahydride 作用下， 以 乙醚 为溶剂， 反应 24.0h， 以91%的产率得到(R)-1'-methyl-[1,3']bipyrrolidine
  参考文献：
  名称：

  Chiral 3-aminopyrrolidines as a rigid diamino scaffold for organocatalysis and organometallic chemistry

  摘要：

  Over 20 new and easily prepared diamines were screened for the asymmetric Morita-Baylis-Hillman reaction. Chiral non-racemic 3-(N,N-dimethylamino)-1-methylpyrrolidine was found to promote efficiently the reaction of methyl vinyl ketone and substituted benzaldehydes. Enantiomeric excesses up to 73% were reached with electron-deficient benzaldehyde derivatives. After a simple deprotonation, one of these diamines was transformed into a chiral mixed aggregate for the enantioselective synthesis of (R)-1-o-tolylethanol with 76% ee. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetasy.2010.04.038

文献信息

• [EN] 2-MORPHOLINO-4-PYRIMIDONE COMPOUND<br/>[FR] COMPOSE 2-MORPHOLINO-4-PYRIMIDONE
  申请人：MITSUBISHI PHARMA CORP

  公开号：WO2006028290A1

  公开（公告）日：2006-03-16

  A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; 1 represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R' represents a C1-C6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C1-C6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

  化合物的化学式（I）所代表的化合物，其光学活性异构体，或其药用可接受盐：其中X代表CH或N；1代表C1-C12烷基；R2代表氢原子，或类似物；R'代表C1-C6烷基或类似物；q代表0或1至7的整数；Y代表C1-C6烷基或类似物；p代表0或1至5的整数；R代表2,3-二氢吲哚基或类似物，用于预防和/或治疗由tau蛋白激酶1过度活化引起的疾病，如神经退行性疾病（例如阿尔茨海默病）。
• [EN] COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY<br/>[FR] COMPOSÉS POUR LE TRAITEMENT D'UNE AMYOTROPHIE SPINALE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2016184832A1

  公开（公告）日：2016-11-24

  The present invention provides compounds of formula (I) wherein A, X, Y, R1 and R2 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.

  本发明提供了如下式（I）中的化合物，其中A、X、Y、R1和R2如本文所述，以及其药学上可接受的盐。此外，本发明涉及制造如式（I）中的化合物，包括含有它们的药物组合物以及它们作为药物的用途。
• Organic Compounds
  申请人：Fairhurst Robin Alec

  公开号：US20100286126A1

  公开（公告）日：2010-11-11

  A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R 1 , R 2 and R 3 are as defined herein.

  化合物的公式（I）或其立体异构体或药用可接受的盐，以及它们的制备和用途作为药物，其中R1、R2和R3如本文所定义。
• [EN] IMIDAZO[1,2-A]PYRAZIN-1YL-BENZAMIDE COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY<br/>[FR] COMPOSÉS IMIDAZO[1,2-A]PYRAZIN-1YL-BENZAMIDE POUR LE TRAITEMENT DE L'AMYOTROPHIE SPINALE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2015197503A1

  公开（公告）日：2015-12-30

  The present invention provides compounds of formula (I) wherein A, Xl, X2, R1, R2, R3, R4and R5are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of spinal muscular atrophy.

  本发明提供了式（I）的化合物，其中A、Xl、X2、R1、R2、R3、R4和R5如本文所述，以及其药学上可接受的盐。此外，本发明涉及制备式（I）的化合物、包含它们的药物组合物及其作为治疗脊髓性肌萎缩症的药物的用途。
• 2-MORPHOLINO-4-PYRIMIDONE COMPOUND
  申请人：WATANABE Kazutoshi

  公开号：US20090124618A1

  公开（公告）日：2009-05-14

  A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C 1 -C 12 alkyl; R 2 represents a hydrogen atom, or the like; R′ represents a C 1 -C 6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C 1 -C 6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

  化合物的化学式为（I），其手性异构体或药物可接受的盐：其中X代表CH或N；代表C1-C12烷基；R2代表氢原子或类似物；R'代表C1-C6烷基或类似物；q代表0或1至7的整数；Y代表C1-C6烷基或类似物；p代表0或1至5的整数；R代表2,3-二氢吲哚基或类似物，用于预防和/或治疗由tau蛋白激酶1过度活化引起的疾病，例如神经退行性疾病（例如阿尔茨海默病）。