22462-40-4Relevant articles and documents
Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1
Ambler, Catherine M.,Arnold, Eric,Banker, Mary Ellen,Clark, James D.,Dowty, Martin E.,Efremov, Ivan V.,Fensome, Andrew,Flick, Andrew,Gerstenberger, Brian S.,Gifford, Roger S.,Gopalsamy, Ariamala,Hegen, Martin,Jussif, Jason,Limburg, David C.,Lin, Tsung H.,Pierce, Betsy S.,Sharma, Raman,Trujillo, John I.,Vajdos, Felix F.,Vincent, Fabien,Wan, Zhao-Kui,Xing, Li,Yang, Xiaojing,Yang, Xin
supporting information, (2020/04/15)
Herein, we disclose a new series of TYK2/ JAK1 inhibitors based upon a 3.1.0 azabicyclic substituted pyrimidine scaffold. We illustrate the use of structure-based drug design for the initial design and subsequent optimization of this series of compounds. One advanced example 19 met program objectives for potency, selectivity and ADME, and demonstrated oral activity in the adjuvant-induced arthritis rat model.
Chemoselectivity and Regoselectivity in Reactions of Pyrimidines
Gacek, Michel,Undheim, Kjell
, p. 691 - 696 (2007/10/02)
Selective nucleophilic substitution and hydrogenolysis reactions in pyrimidines are discussed.Stepwise oxidation reactions of pyrimidine sulfides and HPLC studies of these are reported.
