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
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。