3-pyrrolidino-1-(2'-aminophenyl)propane-1-one | 177611-50-6

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 3-pyrrolidino-1-(2'-aminophenyl)propane-1-one
• 英文别名: 1-(2-Aminophenyl)-3-pyrrolidin-1-ylpropan-1-one
• CAS: 177611-50-6
• 化学式: C₁₃H₁₈N₂O
• 分子量: 218.299
• InChiKey: MUMUDFZUKMKFRR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  16
• 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：
  46.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-乙基-7,8-二氢-4-羟基-1H-吡喃并[3,4-f]吲嗪-3,6,10(4H)-三酮 、 3-pyrrolidino-1-(2'-aminophenyl)propane-1-one 在 对甲苯磺酸 作用下， 以 甲苯 为溶剂， 以40%的产率得到4-Ethyl-4-hydroxy-11-(2-pyrrolidin-1-yl-ethyl)-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione
  参考文献：
  名称：

  Synthesis and antitumor activity of 7-substituted 20(RS)-camptothecin analogues

  摘要：

  Novel water-soluble camptothecin analogues with excellent antitumor activity have been designed and synthesized by total synthesis. The analogues were evaluated for cytotoxic activity against five tumor cell lines. The most potent analogue 6c exhibited significant antitumor activity at wider range of doses as compared with camptothecin (T/C 243 % at 70mg/kg; T/C > 150% at 8.75-140mg/kg). Copyright (C) 1996 Elsevier Science Ltd

  DOI：

  10.1016/0960-894x(96)00131-x
• 作为产物：
  描述：

  3-pyrrolidino-1-(2'-nitrophenyl) propane-1-one 在 sodium dithionite 作用下， 以 乙醇 为溶剂， 生成 3-pyrrolidino-1-(2'-aminophenyl)propane-1-one
  参考文献：
  名称：

  Synthesis and antitumor activity of 7-substituted 20(RS)-camptothecin analogues

  摘要：

  Novel water-soluble camptothecin analogues with excellent antitumor activity have been designed and synthesized by total synthesis. The analogues were evaluated for cytotoxic activity against five tumor cell lines. The most potent analogue 6c exhibited significant antitumor activity at wider range of doses as compared with camptothecin (T/C 243 % at 70mg/kg; T/C > 150% at 8.75-140mg/kg). Copyright (C) 1996 Elsevier Science Ltd

  DOI：

  10.1016/0960-894x(96)00131-x

文献信息

• CAMPTOTHECIN DERIVATIVES AND ITS MANUFACTURING METHOD
  申请人：CHONG KUN DANG CORP

  公开号：EP0802915B1

  公开（公告）日：2002-12-04
• US6177568B1
  申请人：——

  公开号：US6177568B1

  公开（公告）日：2001-01-23
• US6265413B1
  申请人：——

  公开号：US6265413B1

  公开（公告）日：2001-07-24
• [EN] CAMPTOTHECIN DERIVATIVES AND ITS MANUFACTURING METHOD<br/>[FR] DERIVES DE CAMPTOTHECINE ET LEUR PROCEDE DE FABRICATION
  申请人：CHONG KUN DANG CORPORATION

  公开号：WO1996021666A1

  公开（公告）日：1996-07-18

  (EN) This invention relates to camptothecin derivatives and pharmaceutically acceptable salts thereof, its manufacturing method and antineoplastic agent containing it. The compound of this invention is camptothecin derivatives modified in B-ring and E-ring thus show improved water solubility and enhanced antineoplastic effect.(FR) Dérivés de camptothécine, leurs sels pharmaceutiquement acceptables, leur procédé de fabrication, et agent antinéoplasique les contenant. Les composés de l'invention sont des dérivés de camptothécine modifiés au niveau des noyaux B et E, ce qui améliore leur hydrosolubilité et leur action antinéoplasique.
• Synthesis and antitumor activity of 7-substituted 20(RS)-camptothecin analogues
  作者：Sang-sup Jew、Hee-Jin Kim、Myoung Goo Kim、Eun-Young Roh、Youn-sang Cho、Joon-Kyum Kim、Kyung-Hoe Cha、Kang-Keun Lee、Hyun-Jung Han、Jae-Young Choi、Heesoon Lee

  DOI：10.1016/0960-894x(96)00131-x

  日期：1996.4

  Novel water-soluble camptothecin analogues with excellent antitumor activity have been designed and synthesized by total synthesis. The analogues were evaluated for cytotoxic activity against five tumor cell lines. The most potent analogue 6c exhibited significant antitumor activity at wider range of doses as compared with camptothecin (T/C 243 % at 70mg/kg; T/C > 150% at 8.75-140mg/kg). Copyright (C) 1996 Elsevier Science Ltd