4-acetoxymethyl-11-acetyl-9-hydroxy-8-methylene-14-oxa-1,11-diazatetracyclo[7.4.1.02,7.010,12 ]tetradeca-2,4,6-trien-6-yl acetate | 102409-58-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 4-acetoxymethyl-11-acetyl-9-hydroxy-8-methylene-14-oxa-1,11-diazatetracyclo[7.4.1.02,7.010,12 ]tetradeca-2,4,6-trien-6-yl acetate
• 英文别名: 4-Acetoxymethyl-11-acetyl-9-hydroxy-8-methylene-14-oxa-1,11-diazatetracyclo[7.4.1.02,7.010,12]tetradeca-2,4,6-trien-6-yl acetate；(11-acetyl-6-acetyloxy-9-hydroxy-8-methylidene-14-oxa-1,11-diazatetracyclo[7.4.1.02,7.010,12]tetradeca-2(7),3,5-trien-4-yl)methyl acetate
• CAS: 102409-58-5
• 化学式: C₁₉H₂₀N₂O₇
• 分子量: 388.377
• InChiKey: CRTALHCFHHLOHA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  28
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  105
• 氢给体数：
  1
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  4-hydroxymethyl-8-methylene-14-oxa-1,11-diazatetracyclo[7.4.1.02,7.010,12 ]tetradeca-2,4,6-triene-6,9-diol 、 乙酸酐 在 甲醇 、 氯仿 作用下， 以 吡啶 为溶剂， 反应 16.0h， 以v/v) to give 4-acetoxymethyl-11-acetyl-9-hydroxy-8-methylene-14-oxa-1,11-diazatetracyclo[7.4.1.02,7.010,12 ]tetradeca-2,4,6-trien-6-yl acetate (6 mg)的产率得到4-acetoxymethyl-11-acetyl-9-hydroxy-8-methylene-14-oxa-1,11-diazatetracyclo[7.4.1.02,7.010,12 ]tetradeca-2,4,6-trien-6-yl acetate
  参考文献：
  名称：

  Biologically pure culture of Streptomyces sandaensis No. 6897

  摘要：

  本文披露了一种能够产生抗肿瘤和抗微生物化合物FR-900482的Streptomyces sandaensis的生物纯培养物。

  公开号：

  US04743555A1

文献信息

• Tetracyclo compounds and a pharmaceutical composition containing the same
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US04645765A1

  公开（公告）日：1987-02-24

  New tetracyclo compounds of the formula: ##STR1## in which R.sup.1 is formyl, protected formyl, hydroxymethyl, protected hydroxymethyl, arylaminomethyl, carboxy, protected carboxy or substituted iminomethyl, R.sup.2 is hydroxy, alkoxy or protected hydroxy, R.sup.3 is hydrogen and R.sup.4 is methyl, hydroxymethyl or protected hydroxymethyl, or R.sup.3 and R.sup.4 are combined together to form methylene or oxo, R.sup.5 is hydroxy, alkoxy or protected hydroxy, and R.sup.6 is hydrogen, imino-protective group or alkyl, and pharmaceutically acceptable salts thereof, which have pharmacological activities such as antitumor activity, antimicrobial activity, and the like, and a process for their production and a pharmaceutical composition containing the same.

  新的四环四氮化合物的化学式为：##STR1## 其中R.sup.1为甲酰基，保护的甲酰基，羟甲基，保护的羟甲基，芳基氨甲基，羧基，保护的羧基或取代的亚胺甲基，R.sup.2为羟基，烷氧基或保护的羟基，R.sup.3为氢，R.sup.4为甲基，羟甲基或保护的羟甲基，或R.sup.3和R.sup.4结合形成亚甲基或氧代基，R.sup.5为羟基，烷氧基或保护的羟基，R.sup.6为氢，亚胺保护基或烷基，以及其药学上可接受的盐。该化合物具有抗肿瘤活性、抗微生物活性等药理活性，并提供了其制备方法和包含该化合物的制药组合物。
• Method of treating tumors using tetracyclo compounds
  申请人：Fujisawa Pharmaceutical Co., Ltd.

  公开号：US04861774A1

  公开（公告）日：1989-08-29

  The invention relates to a method for treatment of carcinoma or sarcoma tumor in mammals which comprises administering to said mammal an effective amount of a tetracyclo compound of the formula: ##STR1## in which R.sup.1 is formyl, protected formyl, hydroxymethyl, protected hydroxymethyl, arylaminomethyl, carboxy, protected carboxy, aryliminomethyl, hydroxyiminomethyl, alkoxyiminomethyl, acyloxyiminomethyl, semicarbazonomethyl or arylsemicarbazonomethyl, R.sup.2 is hydroxy, alkoxy, or protected hydroxy, R.sup.3 is hydrogen and R.sup.4 is methyl, hydroxymethyl or protected hydroxymethyl, or R.sup.3 and R.sup.4 are combined together to form methylene or oxo, R.sup.5 is hydroxy, alkoxy or protected hydroxy, and R.sup.6 is hydrogen, imino-protective group or alkyl, and pharmaceutically acceptable salts thereof.

  本发明涉及一种治疗哺乳动物的癌症或肉瘤肿瘤的方法，其包括向该哺乳动物施用以下式子的四环化合物的有效量：##STR1## 其中R.sup.1是甲酰基，保护的甲酰基，羟甲基，保护的羟甲基，芳基氨甲基，羧基，保护的羧基，芳基亚胺甲基，羟基亚胺甲基，烷氧基亚胺甲基，酰氧基亚胺甲基，半脲甲基或芳基半脲甲基，R.sup.2是羟基，烷氧基或保护的羟基，R.sup.3是氢，R.sup.4是甲基，羟甲基或保护的羟甲基，或R.sup.3和R.sup.4结合形成亚甲基或氧代亚甲基，R.sup.5是羟基，烷氧基或保护的羟基，R.sup.6是氢，亚胺保护基或烷基，以及其药学上可接受的盐。