1H-茚-1,2-二胺,2,3-二氢-,(1S,2S)- | 220998-10-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 1H-茚-1,2-二胺,2,3-二氢-,(1S,2S)-
• 中文别名: 依洛替康
• 英文名称: BN 80927
• 英文别名: Elomotecan；(20R)-6-chloro-20-ethyl-20-hydroxy-7-methyl-10-[(4-methylpiperidin-1-yl)methyl]-17-oxa-3,13-diazapentacyclo[11.9.0.02,11.04,9.015,21]docosa-1(22),2,4(9),5,7,10,15(21)-heptaene-14,18-dione
• CAS: 220998-10-7
• 化学式: C₂₉H₃₂ClN₃O₄
• 分子量: 522.044
• InChiKey: KAQREZSTQZWNAG-GDLZYMKVSA-N

物化性质

• 沸点：
  821.3±65.0 °C(Predicted)
• 密度：
  1.39±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  37
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  83
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  1H-茚-1,2-二胺,2,3-二氢-,(1S,2S)- 以85的产率得到
  参考文献：
  名称：

  Bioorg. Med. Chem. Lett. 1999, 9, 2599-2602

  摘要：

  DOI：
• 作为产物：
  描述：

  (R)-2-[2,7-Dichloro-6-methyl-4-(4-methyl-piperidin-1-ylmethyl)-quinolin-3-ylmethyl]-5-ethyl-5-hydroxy-2,5,6,9-tetrahydro-8-oxa-2-aza-benzocycloheptene-1,7-dione 在 palladium diacetate 、 potassium acetate 、 三苯基膦 作用下， 以 乙腈 为溶剂， 以70%的产率得到1H-茚-1,2-二胺,2,3-二氢-,(1S,2S)-
  参考文献：
  名称：

  BN 80927: A novel homocamptothecin with inhibitory activities on both topoisomerase I and topoisomerase II

  摘要：

  BN 80927, a novel homocamptothecin derivative, inhibits both topoisomerase I and topoisomerase II mediated DNA relaxation and shows pronounced cytotoxicity against HT29, SKOV-3, DU145 and MCF7 human tumor cell lines. (C) 1999 Elsevier Science Ltd. Ail rights reserved.

  DOI：

  10.1016/s0960-894x(99)00428-x

文献信息

• [EN] PHARMACEUTICAL COMPOUNDS FOR THE TREATMENT OF COMPLEMENT MEDIATED DISORDERS<br/>[FR] COMPOSÉS PHARMACEUTIQUES POUR LE TRAITEMENT DE TROUBLES MÉDIÉS PAR LE COMPLÉMENT
  申请人：ACHILLION PHARMACEUTICALS INC

  公开号：WO2020198062A1

  公开（公告）日：2020-10-01

  This disclosure provides pharmaceutical compounds to treat medical disorders, such as complement-mediated disorders, including complement Cl -mediated disorders.

  这份披露提供了用于治疗医学疾病的药物化合物，例如包括补体介导的疾病在内的补体Cl-介导的疾病。
• [EN] CYCLIN-DEPENDENT KINASE INHIBITING COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS<br/>[FR] COMPOSÉS INHIBITEURS DE KINASE DÉPENDANT DE LA CYCLINE POUR LE TRAITEMENT D'AFFECTIONS MÉDICALES
  申请人：G1 THERAPEUTICS INC

  公开号：WO2021236650A1

  公开（公告）日：2021-11-25

  This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.

  这项发明涉及细胞周期抑制化合物领域，用于治疗涉及异常细胞增殖的疾病，包括用于医学治疗的选择性CDK2抑制剂及其药用盐和组合物。
• Product comprising mikanolide, dihydromikanolide or an analogue thereof combine with another anti-cancer agent for therapeutic use in cancer treatment
  申请人：——

  公开号：US20040138245A1

  公开（公告）日：2004-07-15

  The invention concerns a product comprising at least mikanolide, dihydromikanolide or an analogue thereof combined with at least another anti-cancer agent for simultaneous, separate or prolonged therapeutic use in cancer treatment. In a preferred embodiment of the invention, the mikanolide, dihydromikanolide or one analogue thereof is combined with enzymatic inhibitors such as G heterotrimeric protein inhibitors or alkylating agents such as cis-platinum.

  该发明涉及一种产品，其中至少包含米卡酮内酯、二氢米卡酮或其类似物，与至少另一种抗癌药物结合，用于癌症治疗的同时、分开或长期治疗。在该发明的一个优选实施例中，米卡酮内酯、二氢米卡酮或其类似物与酶抑制剂（如G异三聚蛋白抑制剂）或碱化剂（如顺铂）结合。
• Novel Processes for the Production of Useful Intermediates
  申请人：DIOLEZ Christian

  公开号：US20090247563A9

  公开（公告）日：2009-10-01

  The present application relates to a new process for the asymmetric production of 3-(pyridin-4-yl)-3-hydroxy-pentanoic acid derivatives, which are useful intermediates in the manufacture of compounds that are known to show antiproliferative activity.

  本申请涉及一种新的过程，用于不对称生产3-(吡啶-4-基)-3-羟基戊酸衍生物，这些衍生物是制造已知具有抗增殖活性化合物的有用中间体。
• NOVEL PROCESSES FOR THE PRODUCTION OF USEFUL INTERMEDIATES
  申请人：Diolez Christian

  公开号：US20100168426A1

  公开（公告）日：2010-07-01

  The present application relates to a new process for the asymmetric production of 3-(pyridin-4-yl)-3-hydroxy-pentanoic acid derivatives, which are useful intermediates in the manufacture of compounds that are known to show antiproliferative activity.

  本申请涉及一种新的过程，用于不对称生产3-(吡啶-4-基)-3-羟基戊酸衍生物，这些衍生物是制造已知具有抗增殖活性化合物的有用中间体。