Chemoselective reactions of 4,6-dichloro-2-(methylsulfonyl)pyrimidine and related electrophiles with amines
Chemoselective SNAr reactions of 4,6-dichloro-2-(methylsulfonyl) pyrimidine and several related electrophiles with amines and their derivatives are described. In the presence of weak bases anilines and secondary aliphatic amines selectively displace the chloride group. Deprotonated anilines and their carbonyl derivatives displace the sulfone group. Sterically and electronically unbiased primary aliphatic amines selectively displace the sulfone group in 4,6-dichloro-2-(methylsulfonyl)pyrimidine; however, their reactions with other electrophiles generally are less selective. Steric-driven selectivity explanation was proposed. Georg Thieme Verlag Stuttgart. New York.
Baiazitov, Ramil,Du, Wu,Lee, Chang-Sun,Hwang, Seongwoo,Almstead, Neil G.,Moon, Young-Choon
p. 1764 - 1784
(2013/07/26)
Synthesis and biological evaluation of novel pyrimidine derivatives as sub-micromolar affinity ligands of GalR2
GalR1 and GalR2 represent unique pharmacological targets for treatment of seizures and epilepsy. A novel series of 2,4,6-triaminopyrimidine derivatives were synthesized and found to have sub-micromolar affinity for GalR2. Optimization of a series of 2,4,6
Sagi, Vasudeva Naidu,Liu, Tianyu,Lu, Xiaoying,Bartfai, Tamas,Roberts, Edward
scheme or table
p. 7210 - 7215
(2012/01/15)
HETEROARYL COMPOUNDS
This invention relates to compounds of formula (I) their compositions and methods of use thereof. The compounds (and compositions) are useful in modulating IL-12 production and processes mediated by IL-12.
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Page/Page column 99-100
(2010/11/30)
Kinetics of Substitution of 2,4,6-Trichloropyrimidine: Enhanced Reactivity of 2-Chloro Position
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Ramesh, A.,Sundar, B. Syama,Murti, P. S. Radhakrishna
p. 413 - 416
(2007/10/03)
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