动态热力学和动态运动分辨率的2-lithiopyrrolidines的动态热力学和动态运动分辨率
Iain Coldham1, Samuel Dufour, Thomas F N Haxell
1Department of Chemistry, University of Sheffield, Sheffield S3 7HF, UK. i.coldham@sheffield.ac.uk
Journal of the American Chemical Society
|August 17, 2006
概括
这项研究引入了动态分辨率,以创建基丰富的2替代型罗利丁. 研究人员通过使用奇拉配体和有机化合物实现了高分离选择性的罗利丁合成.
科学领域:
- 有机化学 有机化学
- 不对称的合成方法
- 药用化学 医学化学
背景情况:
- 罗利丁衍生物是药品和天然产品中的关键支架.
- 开发有效的方法,以对替代性罗利丁的酶选择性合成是非常可取的.
- 现有的方法往往缺乏广泛的适用性或需要严苛的条件.
研究的目的:
- 开发一种新的动态分辨率策略,用于非对称合成二替代型罗利丁.
- 为了研究N替代剂和性配体对性选择性的影响.
- 探索各种电友的开发方法的范围和局限性.
主要方法:
- 通过锡-交换或去质子化制备种族性2 - Pyrrolidines.
- 动态分辨率通过电友置换在性联结体的存在下.
- 对二聚体复合物的分析和反应动力学.
- 切割N-替代物以产生N-非替代的罗利丁.
主要成果:
- 实现了对racemic 2-lithiopyrrolidines的高度酶选择性电友替代.
- 无论是N-基和N-基的罗利丁衍生物都成功地被分解了.
- 非对称的诱导是通过热力学偏好控制的,对于二聚体复合体.
- N-2,3-二甲基-2-乙烯基衍生物允许高效地切割到N-非替代产品.
- N-Boc-2-lithiopyrrolidine的动态分辨率提供了高不对称的诱导与特定的电友.
结论:
- 动态分辨率是一种有效的策略,用于非对称合成二替代的pyrrolidines.
- 该方法通过选择合适的性配体,可以控制产品的反体.
- 开发的方法可以访问目标罗利丁化合物的两个反体.
- 该策略是多功能性的,可以容纳各种N替代物,并允许获得N不替代的pyrrolidines.
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