通过银介导的利贝斯基德-斯罗格尔合与酸的最小酸的安装
William D Lambert1, Yinzhi Fang1, Subham Mahapatra2
1Department of Chemistry and Biochemistry , University of Delaware , Newark , Delaware 19716 , United States.
Journal of the American Chemical Society
|October 12, 2019
概括
一种新的以银为媒介的交叉合方法可以直接将最小的四基连接到复杂的分子,避免链接,提高安全性. 这种方法增强了生物对角化学应用和探测器开发.
科学领域:
- 有机化学
- 生物对角化学
- 医学化学
背景情况:
- 对复杂分子的生物对角四素的附着通常需要链接剂,这可能会对生理化学性质产生负面影响.
- 传统的四安装方法可能涉及危险的试剂和副产品.
研究的目的:
- 在复杂的分子上安装最小的四基.
- 提高四素合成和应用的安全性和效率.
主要方法:
- 采用一种新的试剂,3-((p-biphenyl-4-ylmethyl) thio) -6-methyltetrazine (b-Tz) 来进行银介导的利贝斯金-斯罗格尔交叉合反应.
- 在温和条件下被PdCl2 ((dppf) 催化.
- 新的试剂 (b-Tz) 设计用于安全的,可扩展的制备,没有素.
主要成果:
- 与传统方法相比,Ag介导的交叉合成功地将最小的,无链接的6-甲基四基功能引入到各种与传统方法相比更高产量的烯酸和烯酸乙烯酸中.
- 合成了一种原四- BODIPY联合体,证明了获得改善.
- 创建了MAGL (单糖醇脂酶) 的共价探针,并用于在活细胞中标记内源MAGL.
结论:
- 开发的Ag介导交叉合方法为直接将四子单元安装在复杂分子上提供了一种多功能且更安全的途径.
- 这种方法预计将通过创建新型结合物和探测器来推进生物对角化学,化学生物学和药物发现.
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