p-fluorophenylcarbaldehyde-tert-butoxycarbonylhydrazone | 149267-64-1

• 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: p-fluorophenylcarbaldehyde-tert-butoxycarbonylhydrazone
• 英文别名: tert-Butyl-2-[(4-fluorophenyl)methylidene]hydrazinecarboxylate；tert-butyl N-[(4-fluorophenyl)methylideneamino]carbamate
• CAS: 149267-64-1
• 化学式: C₁₂H₁₅FN₂O₂
• 分子量: 238.262
• InChiKey: TYZPKUSAKIGNLL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  50.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  p-fluorophenylcarbaldehyde-tert-butoxycarbonylhydrazone 在 N-氯代丁二酰亚胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 以85%的产率得到N′-[chloro-(4-fluorophenyl)methylene]-tert-butylcarbazate
  参考文献：
  名称：

  Synthesis of 5-aryl-3H-[1,3,4]oxadiazol-2-ones from N′-(chloro-aryl-methylene)-tert-butylcarbazates using basic alumina as an efficient and recyclable surface under solvent-free condition

  摘要：

  The synthesis of biologically important 5-aryl-3H-[1,3,4]oxadiazol-2-ones has been carried out by heating the easily synthesized N'-(chloro-aryl-methylene)-tert-butylcarbazates on basic alumina surface under solvent-free condition. The dual characteristic of basic alumina as a solid support as well as a nucleophile is successfully exploited in these reactions. The method provides special attributions such as reduced reaction times, easier work-up procedures, and good to excellent yields as well as increased purity of products and most importantly environmentally friendly protocols. The basic alumina is easily recovered and utilized for further reactions several times without serious loss of activity. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2012.11.128
• 作为产物：
  描述：

  对氟苯甲醛 以 乙醇 为溶剂， 生成 p-fluorophenylcarbaldehyde-tert-butoxycarbonylhydrazone
  参考文献：
  名称：

  Antiretroviral hydrazine derivatives

  摘要：

  本发明涉及具有公式##STR1##的化合物及其盐、药物组合物、中间体及其制备方法。

  公开号：

  US05753652A1

文献信息

• PYRAZOLE COMPOUNDS
  申请人：FUKUMOTO Shoji

  公开号：US20100094000A1

  公开（公告）日：2010-04-15

  The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineralocorticoid receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of a disease or condition mediated by the mineralocorticoid receptor activation.

  本发明涉及其中每个符号如规范中定义的。该化合物具有优越的矿物皮质激素受体拮抗作用，并可用作通过矿物皮质激素受体激活介导的疾病或病况的预防或治疗剂。
• Facile synthesis of potent HIV-1 protease inhibitors containing a novel pseudo-symmetric dipeptide isostere
  作者：Hing L. Sham、David A. Betebenner、Chen Zhao、Norman E. Wideburg、Ayda Saldivar、Dale J. Kempf、Jacob J. Plattner、Daniel W. Norbeck

  DOI：10.1039/c39930001052

  日期：——

  A series of potent inhibitors of the HIV-1 protease containing a novel pseudo-symmetric dipeptide isostere 3 was synthesized via ring opening of a protected epoxide with various substituted hydrazines.

  通过用各种取代的肼将受保护的环氧化物开环，合成了一系列含有新型伪对称二肽等位基因3的有效的HIV-1蛋白酶抑制剂。
• Design, synthesis and antiviral activity of novel pyridazines
  作者：Ziwen Wang、Mingxiao Wang、Xue Yao、Yue Li、Juan Tan、Lizhong Wang、Wentao Qiao、Yunqi Geng、Yuxiu Liu、Qingmin Wang

  DOI：10.1016/j.ejmech.2012.04.020

  日期：2012.8

  A series of pyridazines were prepared and evaluated for their anti-HIV activity. The new synthetic route involving a novel rearrangement reaction provided a practical method for the preparation of 5-hydroxypyridazines. The primary bioassay results indicated that most of the pyridazines possess anti-HIV activity. It ought to been mentioned that the rearranged compounds 35 and 39 exhibited relatively

  制备了一系列哒嗪并评估了它们的抗HIV活性。涉及新颖的重排反应的新的合成途径为制备5-羟基哒嗪提供了一种实用的方法。初步的生物测定结果表明，大多数哒嗪具有抗HIV活性。应该提到的是，重排的化合物35和39表现出相对较高的HIV抑制作用。还发现大多数合成的化合物都具有良好的抗TMV活性，其中化合物9在体内显示出相似的抗TMV活性。对商用植物杀病毒核糖蛋白瑞巴韦林具有抗TMV活性。这项工作提供了一种新的有效方法，可以通过合理整合和优化先前报道的抗病毒剂来开发新型多功能抗病毒剂。
• Antiretroviral hydrazine derivatives
  申请人：Novartis Corporation

  公开号：US05753652A1

  公开（公告）日：1998-05-19

  The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.

  本发明涉及具有公式##STR1##的化合物及其盐、药物组合物、中间体及其制备方法。
• Synthesis of 5-aryl-3H-[1,3,4]oxadiazol-2-ones from N′-(chloro-aryl-methylene)-tert-butylcarbazates using basic alumina as an efficient and recyclable surface under solvent-free condition
  作者：Kamalesh Debnath、Sudipta Pathak、Animesh Pramanik

  DOI：10.1016/j.tetlet.2012.11.128

  日期：2013.2

  The synthesis of biologically important 5-aryl-3H-[1,3,4]oxadiazol-2-ones has been carried out by heating the easily synthesized N'-(chloro-aryl-methylene)-tert-butylcarbazates on basic alumina surface under solvent-free condition. The dual characteristic of basic alumina as a solid support as well as a nucleophile is successfully exploited in these reactions. The method provides special attributions such as reduced reaction times, easier work-up procedures, and good to excellent yields as well as increased purity of products and most importantly environmentally friendly protocols. The basic alumina is easily recovered and utilized for further reactions several times without serious loss of activity. (C) 2012 Elsevier Ltd. All rights reserved.