用可移除的指导组对非替代性基的Palladium (II) -Catalyzed Regioselective syn-Hydroarylation进行反应
Zhen Liu1, Joseph Derosa1, Keary M Engle1
1Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Journal of the American Chemical Society
|September 8, 2016
概括
一种新的催化反应使同质氨酸的区域选择性同质化成为可能. 这种方法有效地产生了许多药物分子中发现的有价值的4,4-非替代的同质氨基基基.
科学领域:
- 有机化学
- 催化剂
- 医学化学
背景情况:
- 同质氨基是药物和生物活性化合物的关键结构基因.
- 复杂有机分子的区域选择性合成仍然是有机化学的一个重大挑战.
研究的目的:
- 开发一种新型的 (II) 催化区域选择性同化反应.
- 使用可切割的双标定向组控制反应选择性.
主要方法:
- (II) 催化被用于水利化反应.
- 使用可切割的双标定向组来控制区域选择性.
- 对各种基进行了反应条件的优化.
主要成果:
- 开发的方法实现了高区域选择性在同质氨酸的同质氨酸.
- 基和基基基底均成功化.
- 这种反应产生了含有4,4-非替代的同质氨基基基的产物.
结论:
- 已经确定了一种新且高效的催化途径到4,4-非替代的同质氨基.
- 使用指导组可以很好地控制反应的选择性.
- 这种方法为合成候选药物和生物活性化合物提供了有价值的工具.
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