| 1018353-38-2

• 分子结构分类: 有机化合物 - 有机氧化合物
• CAS: 1018353-38-2
• 化学式: C₂₉H₂₅N₅OS
• 分子量: 491.616
• InChiKey: RNSLTVATYNZYCV-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  在 镍 、 一水合肼 作用下， 以 甲醇 为溶剂， 反应 0.17h， 以20%的产率得到dimethyl-{4-[4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yloxy]-benzyl}-amine
  参考文献：
  名称：

  Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-β Receptor Type I Inhibitor as Antitumor Agent

  摘要：

  In our continuing effort to expand the SAR of the quinoline domain of dihydropyrrolopyrazole series, we have discovered compound 15d, which demonstrated the antitumor efficacy with oral bioavailability. This effort also demonstrated that the PK/PD in vivo target inhibition paradigm is an effective approach to assess potential for antitumor efficacy. The dihydropyrrolopyrazole inhibitor 15d (LY2109761) is representative of a novel series of antitumor agents.

  DOI：

  10.1021/jm701199p
• 作为产物：
  描述：

  N,N-dimethyl-4-[4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yloxy]-benzamide 在 劳森试剂 作用下， 以 甲苯 为溶剂， 反应 0.75h， 以75%的产率得到
  参考文献：
  名称：

  Optimization of a Dihydropyrrolopyrazole Series of Transforming Growth Factor-β Type I Receptor Kinase Domain Inhibitors: Discovery of an Orally Bioavailable Transforming Growth Factor-β Receptor Type I Inhibitor as Antitumor Agent

  摘要：

  In our continuing effort to expand the SAR of the quinoline domain of dihydropyrrolopyrazole series, we have discovered compound 15d, which demonstrated the antitumor efficacy with oral bioavailability. This effort also demonstrated that the PK/PD in vivo target inhibition paradigm is an effective approach to assess potential for antitumor efficacy. The dihydropyrrolopyrazole inhibitor 15d (LY2109761) is representative of a novel series of antitumor agents.

  DOI：

  10.1021/jm701199p