对于不对称的黄金催化的一点结合配体:具有与TADDOL相关但非循环的脊柱酸
Henrik Teller1, Matthieu Corbet, Luca Mantilli
1Max-Planck-Institut für Kohlenforschung, D-45470 Mülheim/Ruhr, Germany.
Journal of the American Chemical Society
|August 29, 2012
概括
新的非循环胺酸联体使得高分离选择性不对称的黄金催化能够用于各种反应,包括循环添加和循环异构. 这一突破促进了候选药物的高效合成.
科学领域:
- 有机化学 有机化学
- 催化剂是一种催化剂.
- 药用化学 医学化学
背景情况:
- 传统的TADDOL配体使用异乙烯乙部分.
- 新型配体的开发对于推进非对称催化剂至关重要.
研究的目的:
- 开发和评估用于不对称黄金催化而具有非循环骨干的新型胺联体.
- 探索这些连接体在各种有机转化中的作用范围和效率.
- 通过结构和计算研究来合理化催化活动.
主要方法:
- 合成来自TADDOL相关的二醇与非循环脊柱的光胺联体.
- 这些配体在不对称的黄金催化反应中的应用,包括循环添加,循环异构化,利化,胺化和醇化.
- 产品的特征通过enantioselectivity. 产品的特征通过enantioselectivity. 产品的特征通过enantioselectivity.
- 结晶学分析和计算研究,以了解合体 - 金属相互作用.
主要成果:
- 具有非循环脊柱的色胺联体在不对称的黄金催化中表现出色.
- 在一系列机理上不同的反应中实现了高到优异的酶选择性.
- 这些配体在抗抑郁药候选药物 (-) -GSK 1360707.7的合成中得到了成功的应用.
- 结晶学和计算数据提供了有关联体效率的见解.
结论:
- 亚环胺酸联体对于不对称的黄金催化是非常有效的.
- 这些配体为合成具有高立体控制的复杂分子提供了多功能平台.
- 这些发现为合成和药物化学领域的更广泛应用铺平了道路.
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