福米硝唑 | 500-08-3

• 物质功能分类: 原料药 - 抗寄生虫病药 - 抗阿米巴病及抗滴虫病药
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 福米硝唑
• 英文名称: N-(5-nitrothiazol-2-yl)formamide
• 英文别名: N-(5-nitro-thiazol-2-yl)-formamide；N-(5-Nitro-thiazol-2-yl)-formamid；Forminitrazole；N-(5-nitro-1,3-thiazol-2-yl)formamide
• CAS: 500-08-3
• 化学式: C₄H₃N₃O₃S
• mdl: MFCD00866797
• 分子量: 173.152
• InChiKey: ODLJCVGAFRZOOB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  116
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  福米硝唑 、 4-溴丁腈 生成 N-(3-cyano-propyl)-N-(5-nitro-thiazol-2-yl)-formamide
  参考文献：
  名称：

  抗寄生虫5-硝基噻唑和5-硝基-4-噻唑啉。3。

  摘要：

  DOI：

  10.1021/jm00267a016
• 作为产物：
  描述：

  2-氨基-5-硝基噻唑 、 甲乙酐 以 乙醚 为溶剂， 以465 mg的产率得到福米硝唑
  参考文献：
  名称：

  A fluorous and click approach for screening potential PET probes: Evaluation of potential hypoxia biomarkers

  摘要：

  Radiopharmaceuticals for nuclear imaging are essentially targeting molecules, labeled with short-lived radionuclides (e. g., F-18 for PET). A significant drawback of radiopharmaceuticals development is the difficulty to access radiolabeled molecule libraries for initial in vitro evaluation, as radiolabeling has to be optimized for each individual molecule. The present paper discloses a method for preparing libraries of F-18-labeled radiopharmaceuticals using both the fluorous-based F-18-radiochemistry and the Huisgen 1,3-dipolar (click) conjugation reaction. As a proof of concept, this approach allowed us to obtain a series of readily accessible F-18-radiolabeled nitroaromatic molecules, for exploring their structure-activity relationship and further in vitro evaluation of their hypoxic selectivity. Crown Copyright (C) 2011 Published by Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2011.10.084

文献信息

• Derivatives of 2-amino-5-nitrothiazole as potential schistosomicides
  作者：Leslie M. Werbel、Josephine R. Battaglia

  DOI：10.1021/jm00283a004

  日期：1971.1
• Formylation of Amines
  作者：C. W. HUFFMAN

  DOI：10.1021/jo01099a023

  日期：1958.5
• Bushby; Copp, Journal de Pharmacologie, 1955, vol. 7, p. 112,116
  作者：Bushby、Copp

  DOI：——

  日期：——
• A fluorous and click approach for screening potential PET probes: Evaluation of potential hypoxia biomarkers
  作者：Romain Bejot、Laurence Carroll、Kishore Bhakoo、Jérôme Declerck、Veronique Gouverneur

  DOI：10.1016/j.bmc.2011.10.084

  日期：2012.1

  Radiopharmaceuticals for nuclear imaging are essentially targeting molecules, labeled with short-lived radionuclides (e. g., F-18 for PET). A significant drawback of radiopharmaceuticals development is the difficulty to access radiolabeled molecule libraries for initial in vitro evaluation, as radiolabeling has to be optimized for each individual molecule. The present paper discloses a method for preparing libraries of F-18-labeled radiopharmaceuticals using both the fluorous-based F-18-radiochemistry and the Huisgen 1,3-dipolar (click) conjugation reaction. As a proof of concept, this approach allowed us to obtain a series of readily accessible F-18-radiolabeled nitroaromatic molecules, for exploring their structure-activity relationship and further in vitro evaluation of their hypoxic selectivity. Crown Copyright (C) 2011 Published by Elsevier Ltd. All rights reserved.
• Antiparasitic 5-nitrothiazoles and 5-nitro-4-thiazolines. 3
  作者：Peter J. Islip、Michael D. Closier、Martin C. Neville

  DOI：10.1021/jm00267a016

  日期：1973.9