ADN 138 | 99434-90-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶嗪类
• 英文名称: ADN 138
• 英文别名: 8'-Chloro-2',3'-dihydrospiro[pyrrolidine-3,6'(5'H)-pyrrolo-[1,2,3-de][1,4]benzoxazine]-2,5,5'-trione；8'-Chloro-2'3'-dihydrospiro[pyrrolidine-3,6'-pyrrolo[1,2,3-de][1,4]benzoxazine]-2,5,5'(6'H)-trione；8'-Chloro-2',3'-dihydrospiro(pyrrolidine-3,6'(5'H)-pyrrolo(1,2,3-de)(1,4)benzoxazine)-2,5,5'-trione；6-chlorospiro[9-oxa-1-azatricyclo[6.3.1.04,12]dodeca-4(12),5,7-triene-3,3'-pyrrolidine]-2,2',5'-trione
• CAS: 99434-90-9
• 化学式: C₁₃H₉ClN₂O₄
• 分子量: 292.678
• InChiKey: WSLOHMLGIVSUPR-UHFFFAOYSA-N

物化性质

• 熔点：
  271 °C
• 沸点：
  659.0±55.0 °C(Predicted)
• 密度：
  1.71±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  20
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  75.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  ethyl 2-(8-chloro-6-cyano-2,3-dihydro-5-oxo-pyrrolo[1,2,3-de]-1,4-benzoxazine-6-yl)-2-cyanoacetate 以57%的产率得到
  参考文献：
  名称：

  MASUZAWA, KUNIYOSHI;OKAMURA, KYUYA;KASUGA, KAZUNORI;FUJIMORI, SHIZUYOSHI;+

  摘要：

  DOI：

文献信息

• Process for the manufacture of spiro-linked pyrrolidine 2,5-diones
  申请人：Kyorin Pharmaceutical Co., Ltd.

  公开号：US04749789A1

  公开（公告）日：1988-06-07

  This invention relates to novel processes for the manufacture of spiro-linked pyrrolidine-2,5-diones of the formula; ##STR1## which have a potent inhibitory activity on aldose reductase and are useful for reduction and prevention of chronic diabetic complications. The invented processes are useful as improved and convenient method for a large scale manufacture.

  本发明涉及一种新颖的制造spiro-连接的吡咯烷-2,5-二酮的方法，其化学式为; ## STR1 ## 这种化合物具有强大的醛糖还原酶抑制活性，可用于减少和预防慢性糖尿病并发症。发明的方法可作为大规模制造的改进和方便的方法。
• Process for the manufacture of spiro-linked pyrrolidine-2,5-dione
  申请人：Kyorin Pharmaceutical Co., Ltd.

  公开号：US04764608A1

  公开（公告）日：1988-08-16

  This invention relates to novel processes for the manufacture of spiro-linked pyrrolidine-2,5-diones of formula; ##STR1## which have a potent inhibitory activity on aldose reductase and are useful for reduction and prevention of chronic diabetic complications. The invented processes are useful as improved and convenient method for a large scale manufacture.

  本发明涉及一种新型的工艺，用于制造公式为：##STR1## 的螺环联接的吡咯烷-2,5-二酮，该化合物具有对醛糖还原酶的强烈抑制活性，并可用于减少和预防慢性糖尿病并发症。发明的工艺可用作大规模制造的改进和方便的方法。
• 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：——
• MASUDZAVA, KUNIYASU;OKAMURA, XISAYA;FUDZIMORI, SIDZUESI;KINOSITA, SUSUMU;+
  作者：MASUDZAVA, KUNIYASU、OKAMURA, XISAYA、FUDZIMORI, SIDZUESI、KINOSITA, SUSUMU、+

  DOI：——

  日期：——