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Conjugate Additions of Amines to Maleimides via Cooperative Catalysis
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2018-03-07 , DOI: 10.1002/adsc.201800160
Brice E. Uno 1 , Kristine K. Deibler 1 , Carlos Villa 2 , Arjun Raghuraman 2 , Karl A. Scheidt 1
Affiliation  

A cooperative system comprising of a lithium Lewis acid and amine base significantly enhances the rate of the conjugate addition of a wide array of amines to maleimides. This operationally simple, scalable method provides mono‐addition products in high yields and purity. This conjugation was successfully applied to the kinase inhibitor crizotinib in a chemoselective ligation to create novel fluorescent probe.

中文翻译:

通过协同催化将胺加成至马来酰亚胺

包含路易斯酸锂酸和胺碱的协同体系显着提高了多种胺与马来酰亚胺的共轭加成速率。这种操作简单,可扩展的方法可提供高收率和纯度的单加成产物。这种缀合已成功地以化学选择性连接方式应用于激酶抑制剂crizotinib,以创建新型荧光探针。
更新日期:2018-03-07
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