9-chloro-2,3-dihydropyrrolo[1,2,3-de][1,4]benzoxazine-5,6-dione | 99435-17-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 9-chloro-2,3-dihydropyrrolo[1,2,3-de][1,4]benzoxazine-5,6-dione
• 英文别名: 7-Chloro-9-oxa-1-azatricyclo[6.3.1.04,12]dodeca-4(12),5,7-triene-2,3-dione
• CAS: 99435-17-3
• 化学式: C₁₀H₆ClNO₃
• 分子量: 223.616
• InChiKey: KBLTUODYKVYPQB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  9-chloro-2,3-dihydropyrrolo[1,2,3-de][1,4]benzoxazine-5,6-dione 在 N-溴代丁二酰亚胺(NBS) 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以90%的产率得到8-Bromo-9-chloro-2,3-dihydro-[1,4]oxazino[2,3,4-hi]indole-5,6-dione
  参考文献：
  名称：

  Synthesis and antirheumatic activity of novel tetrahydroquinoline-8-carboxylic acid derivatives

  摘要：

  A study of the modification of N-alkylanthranilic acids to develop novel DMARDs is detailed. 1,2,3,4-Tetrahydroquinoline-8-carboxylic acid derivatives were found to exhibit a therapeutic effect on adjuvant arthritis and a suppressive effect on bone destruction. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)00261-8
• 作为产物：
  描述：

  8-氯-3,4-二氢-2H-苯并[1,4]噁嗪 在 吡啶 、 盐酸 、 sodium hydroxide 、 N,N-二甲基-4-亚硝基苯胺 作用下， 以 苯 为溶剂， 生成 9-chloro-2,3-dihydropyrrolo[1,2,3-de][1,4]benzoxazine-5,6-dione
  参考文献：
  名称：

  Synthesis and antirheumatic activity of novel tetrahydroquinoline-8-carboxylic acid derivatives

  摘要：

  A study of the modification of N-alkylanthranilic acids to develop novel DMARDs is detailed. 1,2,3,4-Tetrahydroquinoline-8-carboxylic acid derivatives were found to exhibit a therapeutic effect on adjuvant arthritis and a suppressive effect on bone destruction. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)00261-8

文献信息

• Class of spiro-linked pyrrolidine-2,5-diones
  申请人：Kyorin Pharmaceutical Co., Ltd.

  公开号：US04593092A1

  公开（公告）日：1986-06-03

  The invention provides a novel spiro-linked pyrrolidine-2,5-dione of the formula; ##STR1## wherein X.sub.1 and X.sub.2 each independently represent a hydrogen, a halogen atom, a lower alkyl or lower alkoxy group; Y is a methylene group, oxygen or sulfur atom; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each independently represent a hydrogen atom, a lower alkyl group or forming a benzene ring together with their adjacent carbon atoms; the base salts thereof with pharmaceutically acceptable cations, and processes for their manufactures. The compounds of formula [I] useful as aldose reductase inhibitors and as therapeutic agents for treatment of chronic diabetic complications are also disclosed.

  该发明提供了一种新颖的螺环联接的吡咯烷-2,5-二酮，其化学式为：##STR1## 其中X.sub.1和X.sub.2各自独立地代表氢、卤原子、低碳基或低碳氧基；Y代表亚甲基、氧原子或硫原子；R.sub.1、R.sub.2、R.sub.3和R.sub.4各自独立地代表氢原子、低碳基或与其相邻碳原子共同形成苯环；其与药学上可接受的阳离子形成的盐和其制备方法。还公开了化合物的化学式[I]，用作醛糖还原酶抑制剂和治疗慢性糖尿病并发症的治疗剂。
• Spiro-linked pyrrolidine-2,5-diones and process for their preparation
  申请人：KYORIN PHARMACEUTICAL CO., LTD.

  公开号：EP0147805A2

  公开（公告）日：1985-07-10

  The invention provides a novel spiro-linked pyrrolidine-2,5-dione of the formula;- wherein X1 and X2 each independently represent a hydrogen, a halogen atom, a lower alkyl or lower alkoxy group; Y is a methylene group, oxygen or sulfur atom; R1, R2, R3 and R4 each independently represent a hydrogen atom, a lower alkyl group or forming a benzene ring together with their adjacent carbon atoms; the base salts thereof with pharmaceutically acceptable cations, and processes for their manufactures. The compounds of formula [I] useful as aldose reductase inhibitors and as therapeutic agents for treatment of chronic diabetic complications are also disclosed.

  本发明提供了一种新颖的螺联吡咯烷-2,5-二酮，其式如下 其中X1和X2各自独立地代表氢、卤素原子、低级烷基或低级烷氧基；Y是亚甲基、氧原子或硫原子；R1、R2、R3和R4各自独立地代表氢原子、低级烷基或与其相邻碳原子一起形成苯环；其与药学上可接受的阳离子的基盐及其制造工艺。 还公开了作为醛糖还原酶抑制剂和治疗慢性糖尿病并发症的治疗剂的式[I]化合物。
• IRIKURA, TSUTOMU;TAKANI, XIROKADZU;FUDZIMORI, KIEESI;XIRATA, JOSIXIRO;XIR+
  作者：IRIKURA, TSUTOMU、TAKANI, XIROKADZU、FUDZIMORI, KIEESI、XIRATA, JOSIXIRO、XIR+

  DOI：——

  日期：——
• IRIKURA, TSUTOMU;TAKAGI, KOICHI;FUJIMORI, SHIZUYOSHI;HIRATA, YOSHIHIRO
  作者：IRIKURA, TSUTOMU、TAKAGI, KOICHI、FUJIMORI, SHIZUYOSHI、HIRATA, YOSHIHIRO

  DOI：——

  日期：——
• US4593092A
  申请人：——

  公开号：US4593092A

  公开（公告）日：1986-06-03