(R)-3-Ethylamino-pyrrolidine-1-carboxylic acid tert-butyl ester | 892390-30-6

• 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)-3-Ethylamino-pyrrolidine-1-carboxylic acid tert-butyl ester
• 英文别名: tert-butyl (3R)-3-(ethylamino)pyrrolidine-1-carboxylate
• CAS: 892390-30-6
• 化学式: C₁₁H₂₂N₂O₂
• 分子量: 214.3
• InChiKey: ADWPVFGFNNKQIP-SECBINFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.91
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  (5R,6S)-5,6-bis(4-chlorophenyl)-3-isopropyl-6-methyl-5,6-dihydroimidazo[2,1-b][1,3]thiazole-2-carboxylic acid 、 (R)-3-Ethylamino-pyrrolidine-1-carboxylic acid tert-butyl ester 在 compound 作用下， 生成 tert-butyl (3R)-3-[{[(5R,6S)-5,6-bis(4-chlorophenyl)-3-isopropyl-6-methyl-5,6-dihydroimidazo[2,1-b][1,3]thiazol-2-yl]carbonyl}(ethyl)amino]pyrrolidine-1-carboxylate
  参考文献：
  名称：

  Imidazothiazole derivatives

  摘要：

  提供了一种新的化合物，它抑制小鼠双分子分钟2（Mdm2）蛋白与p53蛋白之间的相互作用，并展现出抗肿瘤活性。本发明提供了一种咪唑噻唑衍生物，其表示为以下公式（1），具有各种取代基，可抑制Mdm2蛋白与p53蛋白之间的相互作用并展现出抗肿瘤活性：其中，公式（1）中的R1、R2、R3、R4和R5每个都具有规范中定义的相同含义。

  公开号：

  US20090312310A1

文献信息

• Method for Production of Optically Active 3-Amino-Nitrogenated Compound
  申请人：Ohnuki Masatoshi

  公开号：US20090326246A1

  公开（公告）日：2009-12-31

  Aiming at production of an optically active 3-amino nitrogen-containing compound which is useful as an intermediate in synthesis of medicines and pesticides, in particular, an optically active 1-protected-3-aminopyrrolidine derivative, from an inexpensive and readily available raw material by a process which is efficient and can be practiced industrially, an optically active 3-amino nitrogen-containing compound is produced by performing a reaction of an optically active 3-substituted nitrogen-containing compound with ammonia, methylamine, ethylamine or dimethylamine in the presence of water. In addition, a 1-protected-3-aminopyrrolidine derivative is produced by performing a reaction of an optically active 1-protected-3-(sulfonyloxy)pyrrolidine derivative with ammonia, methylamine, ethylamine, or dimethylamine in the presence of methanol, ethanol, n-propanol, or isopropanol under a pressure of less than 30 barr.

  本发明旨在从一种廉价且易得的原材料出发，通过一种高效且可工业化实践的方法，制备一种光学活性的3-氨基含氮化合物，该化合物在合成药物和杀虫剂中作为中间体特别有用，特别是一种光学活性的1-保护-3-氨基吡咯烷衍生物。该方法包括在水的存在下，将光学活性的3-取代氮含化合物与氨、甲基胺、乙基胺或二甲胺反应，从而制备一种光学活性的3-氨基含氮化合物。此外，通过在甲醇、乙醇、正丙醇或异丙醇的存在下，在小于30巴的压力下，将光学活性的1-保护-3-(磺酰氧基)吡咯烷衍生物与氨、甲基胺、乙基胺或二甲胺反应，从而制备一种1-保护-3-氨基吡咯烷衍生物。
• METHOD FOR PRODUCTION OF OPTICALLY ACTIVE 3-AMINO-NITROGENATED COMPOUND
  申请人：Kaneka Corporation

  公开号：EP2050735A1

  公开（公告）日：2009-04-22

  Aiming at production of an optically active 3-amino nitrogen-containing compound which is useful as an intermediate in synthesis of medicines and pesticides, in particular, an optically active 1-protected-3-aminopyrrolidine derivative, from an inexpensive and readily available raw material by a process which is efficient and can be practiced industrially, an optically active 3-amino nitrogen-containing compound is produced by performing a reaction of an optically active 3-substituted nitrogen-containing compound with ammonia, methylamine, ethylamine or dimethylamine in the presence of water. In addition, a 1-protected-3-aminopyrrolidine derivative is produced by performing a reaction of an optically active 1-protected-3-(sulfonyloxy)pyrrolidine derivative with ammonia, methylamine, ethylamine, or dimethylamine in the presence of methanol, ethanol, n-propanol, or isopropanol under a pressure of less than 30 barr.

  旨在通过一种高效且可工业化生产的工艺，从廉价且易于获得的原料中生产一种光学活性 3-氨基含氮化合物，该化合物可用作合成药物和杀虫剂的中间体，特别是光学活性 1-保护-3-氨基吡咯烷衍生物、光学活性 3-氨基含氮化合物是通过光学活性 3-取代的含氮化合物与氨、甲胺、乙胺或二甲胺在水的存在下发生反应而制得的。此外，在甲醇、乙醇、正丙醇或异丙醇存在下，在压力小于 30 barr 的条件下，将光学活性的 1-保护-3-（磺酰氧基）吡咯烷衍生物与氨、甲胺、乙胺或二甲胺进行反应，可制得 1-保护-3-氨基吡咯烷衍生物。
• 1-cyano-pyrrolidine compounds as USP30 inhibitors
  申请人：MISSION THERAPEUTICS LIMITED

  公开号：US10343992B2

  公开（公告）日：2019-07-09

  The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (II) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, R10, R12, Z, Y and m are as defined herein.

  本发明涉及新型化合物和去泛素化酶（DUB）抑制剂的制造方法。特别是，本发明涉及泛素 C 端水解酶 30（USP30）的抑制。本发明还涉及 DUB 抑制剂在治疗线粒体功能障碍和癌症方面的用途。本发明的化合物包括具有式(II)的化合物或其药学上可接受的盐，其中R1、R2、R3、R4、R5、R8、R9、R10、R12、Z、Y和m如本文所定义。
• EP3277677B1
  申请人：——

  公开号：EP3277677B1

  公开（公告）日：2021-02-24
• 1-CYANO-PYRROLIDINE COMPOUNDS AS USP30 INHIBITORS
  申请人：Mission Therapeutics Limited

  公开号：EP3277677B9

  公开（公告）日：2021-07-14