dimethylformamide diisopentyl acetal

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 原羧酸衍生物
• 英文名称: dimethylformamide diisopentyl acetal
• 英文别名: N,N-dimethyl-1,1-bis(3-methylbutoxy)methanamine
• 化学式: C₁₃H₂₉NO₂
• 分子量: 231.379
• InChiKey: ROANHWKPRXRERG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  16
• 可旋转键数：
  9
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  21.7
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  cyclo- 、 dimethylformamide diisopentyl acetal 以 甲苯 为溶剂， 反应 4.0h， 以72%的产率得到cyclo-
  参考文献：
  名称：

  Derivatives of a Novel Cyclopeptolide. 2. Synthesis, Activity against Multidrug Resistance in CHO and KB Cells in vitro, and Structure-Activity Relationships

  摘要：

  A series of derivatives of the novel cyclopeptolide 1 was prepared, and their ability to chemosensitize multi drug resistant CHO and KB cells in vitro was evaluated. In contrast to the parent compound, several of the derivatives were found to be highly active. In particular, conversion of the R-lactic acid residue of 1 into its S-isomer via lactone ring cleavage and recyclization with inversion resulted in a marked enhancement of activity. Some of these derivatives (e.g., 15a, SDZ 280.446) belong to the most potent resistance modulating compounds known so far.

  DOI：

  10.1021/jm00039a003
• 作为产物：
  描述：

  异戊醇 、 N,N-二甲基甲酰胺二甲基缩醛 以85%的产率得到dimethylformamide diisopentyl acetal
  参考文献：
  名称：

  Derivatives of a Novel Cyclopeptolide. 2. Synthesis, Activity against Multidrug Resistance in CHO and KB Cells in vitro, and Structure-Activity Relationships

  摘要：

  A series of derivatives of the novel cyclopeptolide 1 was prepared, and their ability to chemosensitize multi drug resistant CHO and KB cells in vitro was evaluated. In contrast to the parent compound, several of the derivatives were found to be highly active. In particular, conversion of the R-lactic acid residue of 1 into its S-isomer via lactone ring cleavage and recyclization with inversion resulted in a marked enhancement of activity. Some of these derivatives (e.g., 15a, SDZ 280.446) belong to the most potent resistance modulating compounds known so far.

  DOI：

  10.1021/jm00039a003

文献信息

• Pipecolic acid containing cyclopeptolides, their preparation and pharmaceutical compositions containing them
  申请人：SANDOZ AG

  公开号：EP0360760A2

  公开（公告）日：1990-03-28

  Pipecolic acid-containing peptolides wherein the peptidic backbone is of at least 9 a-amino acid residues joined together by peptide bonds, particularly the compounds of formula I wherein the substituents have various significances, are disclosed. They can be prepared by isolation or derivation from an appropriate microorganism strain such as S 42508/F (NRRL 15761). They have interesting pharmacological, e.g. antifungal, chemotherapeutic drug resistance reversing and to some extent immunosuppressant and antiinflammatory properties.

  含联哌羧酸的多肽，其中肽骨架由至少 9 个通过肽键连接在一起的 a-氨基酸残基组成，特别是式 I 的化合物 其中的取代基具有各种意义。 它们可以通过从适当的微生物菌株（如 S 42508/F（NRRL 15761））中分离或衍生制备。 它们具有有趣的药理特性，例如抗真菌、逆转化疗药物耐药性，以及在一定程度上的免疫抑制和抗炎特性。
• US5643869A
  申请人：——

  公开号：US5643869A

  公开（公告）日：1997-07-01
• Derivatives of a Novel Cyclopeptolide. 2. Synthesis, Activity against Multidrug Resistance in CHO and KB Cells in vitro, and Structure-Activity Relationships
  作者：Gerhard Emmer、Maximilian A. Grassberger、Gerhard Schulz、Danielle Boesch、Claire Gaveriaux、Francis Loor

  DOI：10.1021/jm00039a003

  日期：1994.6

  A series of derivatives of the novel cyclopeptolide 1 was prepared, and their ability to chemosensitize multi drug resistant CHO and KB cells in vitro was evaluated. In contrast to the parent compound, several of the derivatives were found to be highly active. In particular, conversion of the R-lactic acid residue of 1 into its S-isomer via lactone ring cleavage and recyclization with inversion resulted in a marked enhancement of activity. Some of these derivatives (e.g., 15a, SDZ 280.446) belong to the most potent resistance modulating compounds known so far.