通过单电子还原实现的化酶的不对称化
Max R Friedfeld1, Hongyu Zhong1, Rebecca T Ruck2
1Department of Chemistry, Princeton University, Princeton, NJ 08544, USA.
概括
一种新的激活方法使用-催化剂实现了高效的不对称化. 这一突破为合成诸如莱维他之类的重要药物提供了成本高效的替代品.
科学领域:
- 催化剂
- 有机金属化学
- 不对称的合成
背景情况:
- 开发一线过渡金属催化剂的性能与贵金属相美至关重要.
- 一个电子化学提供了潜力,
研究的目的:
- 识别利用单电子化学的催化剂激活模式.
- 在第一排过渡金属催化中克服失活路径.
- 发现高效的-催化剂用于不对称的化.
主要方法:
- 使用与高通量选相容的激活方法.
- 对功能化基的不对称化进行了选.
- 从 (R,R) - Ph-BPE和化物中制备了一个优化的催化剂.
主要成果:
- 许多-组合被确定为不对称的化.
- 优化的催化剂在蛋白质介质中表现出高活性和反选择性.
- 在0. 08%的催化剂负载下成功合成了200克级别的 levetiracetam.
- 立体测量研究显示,促使 (II) 降低到稳定的 (I) 物种.
结论:
- 激活方法对于发现高活性和选择性的-催化剂是有效的.
- 这种方法使得使用土壤丰富的金属高效的不对称合成药物.
- 对激活的机械见解为未来的催化剂设计提供了基础.
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