N-二甲基甲胺:用于二甲基化的一种耐久性,电友性反应剂
Dianhu Zhu1, Yang Gu1, Long Lu1
1Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences , 345 Lingling Road, Shanghai 200032, People's Republic of China.
Journal of the American Chemical Society
|July 17, 2015
概括
一种新型的试剂N-difluoromethylthiophthalimide可以有效地使多种核友分离. 这种方法为在温和条件下引入二甲组提供了新的途径.
科学领域:
- 有机化学
- 合成化学
- 医学化学
背景情况:
- 二甲基 (SCF2H) 组是药物发现中的重要药.
- 开发有效和温和的方法来引入SCF2H组对药物化学至关重要.
研究的目的:
- 开发一种新的,易于使用的电友二甲化试剂.
- 证明开发的试剂对于含有SCF2H的化合物的合成具有广泛的适用性.
主要方法:
- 在四个步骤中从胺和TMSCF2H合成N-difluoromethylthiophthalimide (3).
- 电友二甲基化反应与各种核友,包括酸,胺,醇,β-ketoester,oxindoles和异构.
主要成果:
- 从易于获得的原料中成功合成N-difluoromethylthiophthalimide (3).
- 已证明二甲基化具有广泛的基底范围,涵盖了广泛的核友.
- 在温和的反应条件下实现二甲基化.
结论:
- N-difluoromethylthiophthalimide (3) 是一种强大的多功能电友二甲化试剂.
- 开发的方法为含有有价值的二甲分子的合成提供了有效的途径.
- 这种试剂有助于将SCF2H部分纳入各种有机支架.
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