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通过过氧化物光敏化和Ni介导的基因合实现的C ((sp^{3)) -H甲基化}

Aristidis Vasilopoulos¹, Shane W Krska², Shannon S Stahl³

¹Department of Chemistry, University of Wisconsin, Madison, WI 53706, USA.

Science (New York, N.Y.)

|April 23, 2021

概括

研究人员开发了一种用于药物分子中直接甲基化的新方法. 这种技术利用可见光和过氧化物添加甲基,通过"神奇甲基"效应增强药物特性.

科学领域:

有机化学
医学化学
合成化学

背景情况:

在
魔法甲基
在药物发现中具有关键作用,通过单甲基添加改变药物的效力,选择性和代谢稳定性.
在药物化学中,直接甲基化C(sp3) -H键仍然是一个合成的挑战.

研究的目的:

开发一种新型合成方法,用于药物样分子和制药构件中直接甲基化.

主要方法:

可见光启动的三重能量转移以促进过氧化物同解.
通过β-甲基分裂产生基和随后的原子转移或甲基形成.
基质和甲基的介质交叉合用于直接甲基化.

主要成果:

在多种分子支架中成功地直接甲基化C ((sp3) -H键.
可调节的反应条件和过氧化物替代剂以优化甲基化产量.
证明了一种适用于药物样分子和制药中间体的多功能方法.

结论:

开发的方法提供了有效的甲基化化合物,利用
魔法甲基
对药物优化产生影响.
这种可见光介导的方法在药物化学中提供了一种温和而有效的C(sp3) -H功能化策略.

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