氰化
化学
对映选择合成
激进的
催化作用
戒指(化学)
组合化学
铜
有机化学
药物化学
作者
Lihua Wu,Lei Wang,Pinghong Chen,Yinlong Guo,Guosheng Liu
标识
DOI:10.1002/adsc.202000202
摘要
Abstract A novel approach for enantioselective cyanation of cyclopropanols and their derivatives through copper‐catalyzed radical relay processes has been developed. Various cyclopropanols and cyclopropanone acetals are compatible to the catalytic conditions, providing β‐carbonyl nitriles with excellent enantioselectivity. These products can be readily converted to chiral γ‐amino acids derivatives and drugs such as (R)‐baclofen. Preliminary mechanistic studies have supported a ring‐opening process for cyclopropanoxy radicals followed by copper‐catalyzed enantioselective cyanation of benzylic radicals to form the C−CN bonds in an enantioselective manner. magnified image
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