- Widely Exploited, Yet Unreported: Regiocontrolled Synthesis and the Suzuki–Miyaura Reactions of Bromooxazole Building Blocks
-
An approach to synthesis of 2-, 4-, and 5-bromooxazoles is described. The method was optimized, and its scope was extended to all three isomeric parents, as well as various alkyl- and aryl-substituted bromooxazoles. It was found that direct regiocontrolled lithiation followed by reaction with electrophilic bromine source was common for all substrates and led exclusively to the target substituted 2-, 4- and 5-bromooxazoles on multigram scale. The utility of the multipurpose building blocks obtained in this work was demonstrated in the Suzuki–Miyaura cross-coupling reaction under parallel synthesis conditions.
- Solomin, Vitalii V.,Radchenko, Dmytro S.,Slobodyanyuk, Evgeniy Y.,Geraschenko, Oleksandr V.,Vashchenko, Bohdan V.,Grygorenko, Oleksandr O.
-
p. 2884 - 2898
(2019/03/07)
-
- Compounds and Their Use for Treatment of Amyloid Beta-Related Diseases
-
The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compounds, processes for making said compounds, and their use as medicaments for treatment and/or prevention of Aβ-related diseases.
- -
-
Page/Page column 48
(2012/05/21)
-
- ANTIBACTERIAL AGENTS
-
The present invention is directed to a new class of triazolopyridine derivatives, to their use as antimicrobials, and to pharmaceuticals containing these compounds.
- -
-
Page/Page column 63
(2008/06/13)
-
- A Retro-Diels-Alder Approach to Oxazoles and Imidazoles
-
Heating N-acyl derivatives 4 of 3-endo-aminobicyclohept-5-en-2-endo-ol (3) at 185-195 deg C for 4-5 h provides oxazoles 1a-e in 49-88percent yields.The reaction proceeds via an initial dehydration to an oxazoline which undergoes retro-Diels-Alder reaction to provide the oxazole.Similarly, imidazoles 7a-f may be obtained in 40-79percent yields by heating imidazolines 6a-f to effect the cycloreversion.
- Eissenstat, Michael A.,Weaver, John D.
-
p. 3387 - 3390
(2007/10/02)
-