Iridium‐Catalyzed Asymmetric Allylic Amination with Polar Amines: Access to Building Blocks with Lead‐Like Molecular Properties
Iridium‐Catalyzed Asymmetric Allylic Amination with Polar Amines: Access to Building Blocks with Lead‐Like Molecular Properties
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DOI：
10.1002/adsc.201000721
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发表时间：
2010-12
影响因子：
5.4
通讯作者：
Paolo Tosatti;J. Horn;A. Campbell;D. House;A. Nelson;S. Marsden
中科院分区：
文献类型：
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作者：
Paolo Tosatti;J. Horn;A. Campbell;D. House;A. Nelson;S. Marsden
空气稳定的铱催化剂和偶极非质子溶剂二甲亚砜（DMSO）的组合首次允许在不对称烯丙基取代中系统地利用高极性、官能化胺：获得低分子量、富含sp 3 的手性结构单元，其物理化学性质对于合成铅类小分子具有重要价值。
The combination of an air-stable iridium catalyst and the dipolar aprotic solvent dimethyl sulfoxide (DMSO) allowed, for the first time, the systematic exploitation of highly polar, functionalized amines in asymmetric allylic substitutions: low molecular weight, sp 3 -rich chiral building blocks were obtained with physicochemical properties that will be valuable in the synthesis of lead-like small molecules.