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Conjugate Additions of Amines to Maleimides via Cooperative Catalysis
Author(s) -
Uno Brice E.,
Deibler Kristine K.,
Villa Carlos,
Raghuraman Arjun,
Scheidt Karl A.
Publication year - 2018
Publication title -
advanced synthesis and catalysis
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.541
H-Index - 155
eISSN - 1615-4169
pISSN - 1615-4150
DOI - 10.1002/adsc.201800160
Subject(s) - chemistry , conjugate , combinatorial chemistry , amine gas treating , lewis acids and bases , conjugated system , catalysis , lithium (medication) , chemoselectivity , organic chemistry , polymer , mathematical analysis , mathematics , medicine , endocrinology
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.