Chao Li,Jie Wang,Lisa M. Barton,Shan Yu,Maoqun Tian,David S. Peters,M. N. Satish Kumar,Antony W. Yu,Kristen Johnson,Arnab K. Chatterjee,Ming Yan,Phil S. Baran
出处
期刊:Science [American Association for the Advancement of Science (AAAS)] 日期:2017-04-14卷期号:356 (6342)被引量:342
Swapping boron acids for carbon acids Carbon-bound boronic acids and their esters are widely used as coupling partners to make carbon-carbon bonds. More recently, these chemicals have garnered pharmaceutical interest in their own right. Li et al. report a versatile nickel-catalyzed process to replace carboxylic acids with boronate esters by using a phthalimide activator. The reaction is well suited to late-stage modification of complex molecules. The authors used the approach to produce a potent in vitro inhibitor of human neutrophil elastase, a target of interest in treating inflammatory lung diseases. Science , this issue p. eaam7355