Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-methoxy-4-(5-oxazolyl)phenyl moiety
The first reported structure-activity relationships (SARs) about the N-[3-methoxy-4-(5-oxazolyl)phenyl moiety for a series of recently disclosed inosine monophosphate dehydrogenase (IMPDH) inhibitors are described. The syntheses and in vitro inhibitory values for IMPDH II, and T-cell proliferation (for select analogues) are given.
Iwanowicz, Edwin J.,Watterson, Scott H.,Guo, Junqing,Pitts, William J.,Murali Dhar,Shen, Zhongqi,Chen, Ping,Gu, Henry H.,Fleener, Catherine A.,Rouleau, Katherine A.,Cheney, Daniel L.,Townsend, Robert M.,Hollenbaugh, Diane L.
p. 2059 - 2063
(2007/10/03)
Palladium-Catalyzed Coupling Reactions of (α-Ethoxyvinyl)trimethylstannane with Vinyl and Aryl Triflates
The palladium-catalyzed cross-coupling reaction of vinyl triflates and halides with (α-ethoxyvinyl)trimethylstannane gives high yields of 2-ethoxy 1,3-dienes, which can be hydrolyzed to the corresponding α,β-unsaturated ketones.Aryl triflates undergo an analogous coupling reaction, providing a facile method for replacing the hydroxyl group of a phenol by an acyl group.The use of (α-ethoxyvinyl)trimethylstannane in palladium-catalyzed carbonylative coupling gives rise to vinyl and aryl α-ethoxyvinyl ketones and indirectly to the corresponding α-diketones (which result from their hydrolysis) and glyoxylates (which result from their ozonolysis).