(Z)-3-bromo-2,3-diphenylacrylaldehyde

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: (Z)-3-bromo-2,3-diphenylacrylaldehyde
• 英文别名: (Z)-3-bromo-2,3-diphenylprop-2-enal
• 化学式: C₁₅H₁₁BrO
• 分子量: 287.156
• InChiKey: KPNGVAULLDZMJQ-CCEZHUSRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  17.1
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  (Z)-3-bromo-2,3-diphenylacrylaldehyde 、 2-苯乙酰胺 在 copper(l) iodide 、 caesium carbonate 、 N,N'-二甲基乙二胺 作用下， 以 甲苯 为溶剂， 反应 24.0h， 以50%的产率得到3,5,6-triphenylpyridin-2(1H)-one
  参考文献：
  名称：

  碘化铜（I）催化2-卤代苯甲羰基与2-芳基乙酰胺的级联反应合成喹啉酮

  摘要：

  报道了一种有效的铜催化方法，该方法通过取代的2-碘-，2-溴-和2-氯苯甲酰羰基与2-芳基乙酰胺的级联反应来合成喹啉酮，吡啶酮和杂环吡啶酮。该方案对于大多数2-碘-，2-溴-和2-氯苯甲羰基与2-芳基乙酰胺的反应非常有效。 碘化铜-二胺-级联反应-酰胺化-喹啉酮

  DOI：

  10.1055/s-0030-1259983

文献信息

• Synthesis of azirines containing aldehyde functionality and their utilization as synthetic tools for five membered oxazoles and isoxazoles
  作者：Sulagna Brahma、Jayanta K. Ray

  DOI：10.1002/jhet.5570450203

  日期：2008.3

  A simple and useful procedure for the synthesis of azirines containing aldehyde functionality from open chain bromo/chloro-aldehydes at room temperature is reported. The scope of the ring expansion reaction of a number of 3-substituted-2-formyl-azirines has been examined using different oraganometallic catalysts and a variety of Lewis acids.

  报道了一种在室温下由开链溴/氯醛合成含醛官能团的叠氮基的简单有用的方法。已经使用不同的有机金属催化剂和多种路易斯酸检查了许多3-取代的2-甲酰基-叠氮基的扩环反应的范围。
• [EN] DERIVATIVES OF PYRROLOIMIDAZOLE OR ANALOGUES THEREOF WHICH ARE USEFUL FOR THE TREATMENT OF INTER ALIA CANCER<br/>[FR] DÉRIVÉS DE PYRROLOIMIDAZOLE OU ANALOGUES DE CEUX-CI UTILES, ENTRE AUTRES, DANS LE TRAITEMENT DU CANCER
  申请人：EMCURE PHARMACEUTICALS LTD

  公开号：WO2017134555A1

  公开（公告）日：2017-08-10

  Present invention relates to novel heterocyclic compounds as indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) modulators. Compounds of the present invention inhibit tryptophan degradation by modulating IDO and/or TDO. Formula (I) The invention further relates to the process of their preparation, pharmaceutical composition and their use in modulating the activity of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3- dioxygenase (TDO). The compounds of the invention can be used alone or in combination for the treatment of conditions that benefits from the inhibition of tryptophan degradation.

  本发明涉及作为吲哚胺2,3-二氧化酶（IDO）和/或色氨酸2,3-二氧化酶（TDO）调节剂的新型杂环化合物。本发明的化合物通过调节IDO和/或TDO来抑制色氨酸降解。公式（I）。本发明还涉及它们的制备过程、药物组合物及其在调节吲哚胺2,3-二氧化酶（IDO）和/或色氨酸2,3-二氧化酶（TDO）活性中的应用。本发明的化合物可以单独使用或与其他药物组合用于治疗受益于抑制色氨酸降解的疾病。
• A simple approach to azirines containing an aldehyde functionality and their stabilization as palladium(II) complexes
  作者：Sulagna Brahma、Jayanta K. Ray

  DOI：10.1016/j.tetlet.2005.07.086

  日期：2005.9

  A simple and useful method for the synthesis of azirines containing an aldehyde functionality, from open chain bromo/chloro-aldehydes at room temperature and their stabilization as palladium(II) complexes are reported.

  报道了一种在室温下由开链溴/氯醛合成含醛官能团的叠氮基的简单而有用的方法，该方法稳定了钯（II）配合物。
• Neat synthesis of isothiazole compounds, and studies on their synthetic applications and photophysical properties
  作者：Anirban Bera、Prasanta Patra、Abulkalam Azad、Sk Asraf Ali、Susanta Kumar Manna、Amit Saha、Shubhankar Samanta

  DOI：10.1039/d2nj01962k

  日期：——

  eco-friendly neat synthesis of isothiazoles has been developed for the first time. It is noteworthy that an instantaneous valuable synthetic route of β-enaminones has also been documented during the mechanistic investigation of isothiazole formation. Detail mechanistic explanation of isothaizole formation reaction is clearly explained by the control experiments. NBS promoted aromatisation of isothiazole derivatives

  硫氰酸铵首次开发了促进异噻唑类化合物简单、快速、环保的纯合成。值得注意的是，在异噻唑形成的机理研究过程中，也记录了一条有价值的 β-烯胺酮瞬时合成路线。对照实验清楚地解释了异噻唑形成反应的详细机理解释。NBS 促进了异噻唑衍生物的芳构化，并研究了异噻唑-芘杂化分子的光物理性质。
• DERIVATIVES OF PYRROLOIMIDAZOLE OR ANALOGUES THEREOF WHICH ARE USEFUL FOR THE TREATMENT OF INTER ALIA CANCER
  申请人：EMCURE PHARMACEUTICALS LIMITED

  公开号：US20190031665A1

  公开（公告）日：2019-01-31

  Present invention relates to novel heterocyclic compounds as indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) modulators. Compounds of the present invention inhibit tryptophan degradation by modulating IDO and/or TDO. The invention further relates to the process of their preparation, pharmaceutical composition and their use in modulating the activity of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO). The compounds of the invention can be used alone or in combination for the treatment of conditions that benefits from the inhibition of tryptophan degradation.