3-Cyclopropyl-1-phenyltriazene

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 3-Cyclopropyl-1-phenyltriazene
• 英文别名: N-(cyclopropyldiazenyl)aniline
• 化学式: C₉H₁₁N₃
• 分子量: 161.206
• InChiKey: HQOJGPZMBJKAAB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  12
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  36.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  Azirino[2',3'_3,4]pyrrolo[1,2-.α.]indole-4,7-dione, 1,1a,2,8,8a,8b-hexahydro-6-hydroxy-8-(hydroxymethyl)-8a-methoxy-5-methyl-, 8-carbamate 、 3-Cyclopropyl-1-phenyltriazene 以 二氯甲烷 为溶剂， 反应 1.0h， 以20%的产率得到6-Cyclopropyloxy-6-deaminomitomycin C
  参考文献：
  名称：

  Preparation and antitumor activity of additional mitomycin A analogs

  摘要：

  On the basis of qualitative structure-activity relationships developed in the preceding article, a series of 32 new mitomycin A analogues were prepared and tested in antitumor screens. Seven of them gave greater prolongation of life (ILS) than mitomycin C in the mouse P388 leukemia assay. They included examples with 7-O substituents such as cyclic ethers and nitrogen heterocycles. A Hansch analysis was attempted with log P and MR as the independent variables, but no statistically significant correlation could be made. Seven compounds, chosen mainly for their good potency (MED), were tested in the subcutaneous B16 melanoma assay in mice and four of them showed greater ILS than mitomycin C.

  DOI：

  10.1021/jm00123a036
• 作为产物：
  描述：

  benzenediazonium hexafluorophosphate 、 环丙胺 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 2.0h， 以40%的产率得到3-Cyclopropyl-1-phenyltriazene
  参考文献：
  名称：

  Preparation and antitumor activity of additional mitomycin A analogs

  摘要：

  On the basis of qualitative structure-activity relationships developed in the preceding article, a series of 32 new mitomycin A analogues were prepared and tested in antitumor screens. Seven of them gave greater prolongation of life (ILS) than mitomycin C in the mouse P388 leukemia assay. They included examples with 7-O substituents such as cyclic ethers and nitrogen heterocycles. A Hansch analysis was attempted with log P and MR as the independent variables, but no statistically significant correlation could be made. Seven compounds, chosen mainly for their good potency (MED), were tested in the subcutaneous B16 melanoma assay in mice and four of them showed greater ILS than mitomycin C.

  DOI：

  10.1021/jm00123a036

文献信息

• 6-substituted mitomycin analogs
  申请人：UNIVERSITY PATENTS, INC.

  公开号：EP0324109A2

  公开（公告）日：1989-07-19

  Novel methods for treatment of neoplastic disease states in animals, which methods comprise administering a therapeutically effective amount of a compound of the formula V, wherein: Y is hydrogen or lower alkyl; and X is a radical of the formula -O-R, wherein R is: N,N-di(hydroxy lower alkyl)amino lower alkyl, or tri-lower alkoxy silyl lower alkyl, or cyclo lower alkyl, or halo substituted lower alkoxy lower alkyl, or tetrahydro pyranyl, or carboethoxy lower alkyl, or 1-lower alkyl pyrrolidinyl lower alkyl, or N-pyrrolidinyl lower alkyl, or 1-lower alkyl pyrrolydinyl, or dioxanyl, or hydroxy lower alkenyl, or hydroxy lower alkyl thio lower alkyl thio lower alkyl, or dioxanyl lower alkyl, or lower alkyl thio lower alkyl, or phenyl thio lower alkyl, or phenoxy lower alkyl, or thiophenyl lower alkyl, or 1-lower alkyl piperidyl, or alkyl carbonyl amino alkyl, or N-­piperidyl lower alkyl, or lower alkoxy lower alkyl or lower alkyl thio hydroxy lower alkyl, or 1-lower alkyl N-­piperazinyl lower alkyl, or N-thiomorpholinyl lower alkyl.

  治疗动物肿瘤性疾病状态的新方法，该方法包括施用治疗有效量的式 V 化合物、 其中Y 是氢或低级烷基；X 是式 -O-R 的基团，其中 R 是： N,N-二(羟基低级烷基)氨基低级烷基，或三低级烷氧基硅基低级烷基，或环低级烷基，或卤代低烷氧基低级烷基，或四氢吡喃基，或羧氧基低级烷基，或 1-吡咯烷基低级烷基，或 N-吡咯烷基低级烷基，或 1-吡咯烷基低级烷基，或二噁烷基，或羟基低级烯基，或羟基低级烷基硫代低级烷基硫代低级烷基、或二噁烷基低级烷基，或低级烷基硫代低级烷基，或苯基硫代低级烷基，或苯氧基低级烷基，或噻吩基低级烷基，或 1-低级哌啶基烷基，或烷基羰基氨基烷基，或 N-哌啶基低级烷基，或低级烷氧基低级烷基，或低级烷基硫代羟基低级烷基，或 1-低级哌嗪基低级烷基，或 N-硫代吗啉基低级烷基。
• SAMI, SALAH M.;REMERS, WILLIAM A.;BRADNER, WILLIAM T., J. MED. CHEM., 32,(1989) N, C. 703-708
  作者：SAMI, SALAH M.、REMERS, WILLIAM A.、BRADNER, WILLIAM T.

  DOI：——

  日期：——
• US5023253A
  申请人：——

  公开号：US5023253A

  公开（公告）日：1991-06-11
• WO1989005811A1
  申请人：——

  公开号：WO1989005811A1

  公开（公告）日：1989-06-29
• Preparation and antitumor activity of additional mitomycin A analogs
  作者：Salah M. Sami、William A. Remers、William T. Bradner

  DOI：10.1021/jm00123a036

  日期：1989.3

  On the basis of qualitative structure-activity relationships developed in the preceding article, a series of 32 new mitomycin A analogues were prepared and tested in antitumor screens. Seven of them gave greater prolongation of life (ILS) than mitomycin C in the mouse P388 leukemia assay. They included examples with 7-O substituents such as cyclic ethers and nitrogen heterocycles. A Hansch analysis was attempted with log P and MR as the independent variables, but no statistically significant correlation could be made. Seven compounds, chosen mainly for their good potency (MED), were tested in the subcutaneous B16 melanoma assay in mice and four of them showed greater ILS than mitomycin C.