89143-20-4Relevant articles and documents
Conjugate Additions of Amines to Maleimides via Cooperative Catalysis
Uno, Brice E.,Deibler, Kristine K.,Villa, Carlos,Raghuraman, Arjun,Scheidt, Karl A.
, p. 1719 - 1725 (2018)
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. (Figure presented.).