8-fluoro-10H-benzo[b]pyrido[2,3-e][1,4] oxazine | 1370030-93-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 8-fluoro-10H-benzo[b]pyrido[2,3-e][1,4] oxazine
• 英文别名: 8-fluoro-10H-pyrido[3,2-b][1,4]benzoxazine
• CAS: 1370030-93-5
• 化学式: C₁₁H₇FN₂O
• 分子量: 202.188
• InChiKey: QNRWOYDFPVYFRF-UHFFFAOYSA-N

物化性质

• 熔点：
  240-243 °C
• 沸点：
  336.3±42.0 °C(predicted)
• 密度：
  1.342±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  34.2
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  8-fluoro-10H-benzo[b]pyrido[2,3-e][1,4] oxazine 、 tert-butyl (3,6-dihydro-2H-pyran-3-yl) carbonate 在 tris(dibenzylideneacetone)dipalladium(0) chloroform complex 、 (1R,2R)-(+)-1,2-二氨基环己烷-N,N′-双(2-二苯基磷苯甲酰) 作用下， 以 二氯甲烷 为溶剂， 反应 240.0h， 生成 (R)-10-(3,6-dihydro-2H-pyran-3-yl)-8-fluoro-10H-benzo[b]pyrido[2,3-e][1,4]oxazine
  参考文献：
  名称：

  [EN] STEREOSPECIFIC PROCESS FOR 3-HETEROCYCLYLCYCLOALIPHATIC-1,2-DIOLS
  [FR] PROCÉDÉ STÉRÉOSPÉCIFIQUE POUR DIOLS 3-HETEROCYCLYLCYCLOALIPHATIQUES-1,2

  摘要：

  公开号：

  WO2017024229A8
• 作为产物：
  描述：

  3-羟基-2-碘吡啶 在 tin(II) chloride dihdyrate 、 potassium carbonate 、 N,N'-二甲基乙二胺 作用下， 以 二甲基亚砜 、 乙酸乙酯 、 甲苯 为溶剂， 反应 42.0h， 生成 8-fluoro-10H-benzo[b]pyrido[2,3-e][1,4] oxazine
  参考文献：
  名称：

  Transition-Metal-Free Intramolecular N-Arylations

  摘要：

  N-Substituted phenoxazines and related aza analogs have been prepared from N-acetylated aryloxy anilides by transition-metal-free, base-catalyzed cyclization reactions. In the presence of a mixture of 10 mol % of N,N-dimethylethylenediamine (DMEDA) and 2 equiv of K2CO3 in toluene at 135 degrees C the products are obtained in high yields.

  DOI：

  10.1021/ol3005134

文献信息

• Compositions and methods for treating cancer
  申请人：CASE WESTERN RESERVE UNIVERSITY

  公开号：US10744141B2

  公开（公告）日：2020-08-18

  A method of treating cancer in a subject in need thereof includes administering to the subject therapeutically effective amounts of a PP2A activator and a protein kinase inhibitor.

  一种治疗有需要的受试者癌症的方法，包括向受试者施用治疗有效量的 PP2A 激活剂和蛋白激酶抑制剂。
• Heterocyclic constrained tricyclic sulfonamides as anti-cancer agents
  申请人：ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

  公开号：US10759790B2

  公开（公告）日：2020-09-01

  A genus of arylsulfonamide derivatives of heterocyclic constrained tricyclic compounds is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a therapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.

  本发明公开了一种杂环受限三环化合物的芳基磺酰胺衍生物。这些化合物属 这些化合物通过调节 PP2A 诱导 FOXO1 转录因子转位到细胞核，因此具有抗增殖作用。它们可用于治疗多种疾病，包括癌症治疗，或与其他药物联合使用，以恢复对已产生抗药性的化疗的敏感性。
• HETEROTRICYCLIC SULFONAMIDES AS ANTI-CANCER AGENTS
  申请人：Icahn School of Medicine at Mount Sinai

  公开号：EP3347355B1

  公开（公告）日：2022-07-13
• SULFONAMIDES DERIVED FROM TRICYCLYL-2-AMINOCYCLOALKANOLS AS ANTICANCER AGENTS
  申请人：ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI

  公开号：US20170015625A1

  公开（公告）日：2017-01-19

  A genus of arylsulfonamide derivatives of aminocycloalkanols is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
• US9937186B2
  申请人：——

  公开号：US9937186B2

  公开（公告）日：2018-04-10