Lewis Acid-Catalyzed Generation of CC and CN Bonds on π-Deficient Heterocyclic Substrates
作者:Matteo Staderini、Maria Laura Bolognesi、J. Carlos Menéndez
DOI:10.1002/adsc.201400674
日期:2015.1.12
to the efficient and completely regioselective generation of aromatic CC and CNbonds. The method is simple, rapid, general and inexpensive, and can be performed without the use of dried solvents. Most of the synthetized compounds are new and in many cases the work‐up required only filtration. Furthermore, this is the first example of the use of a Lewis acid as a catalyst for heteroarylation, vinylation
QUINAZOLINE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF DIABETES AND OBESITY
申请人:Lee Nam Kyu
公开号:US20080207614A1
公开(公告)日:2008-08-28
The present invention relates to novel quinazoline derivatives effective in lowering blood glucose level and body weight, and a medicine for treatment and/or prevention of diabetes and/or obesity, which comprises the compound as an active ingredient.
The Scope and Mechanism of Phosphonium-Mediated S<sub>N</sub>Ar Reactions in Heterocyclic Amides and Ureas
作者:Zhao-Kui Wan、Sumrit Wacharasindhu、Christopher G. Levins、Melissa Lin、Keiko Tabei、Tarek S. Mansour
DOI:10.1021/jo7020373
日期:2007.12.1
An efficient “one-step” synthesis of cyclic amidines and guanidines has been developed. Treatment of cyclic amides and ureas with benzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP), base, and nitrogen nucleophiles leads to the formation of the corresponding cyclic amidines and guanidines, typically in good to excellent yields. This method has also been used to prepare heteroaryl
[graphics]An efficient one-step amination of cyclic amides and ureas has been developed. Treatment of cyclic amides and cyclic ureas with BOP in the presence of DBU in various solvents led to the formation of cyclic amidines and cyclic guanidines in good to excellent yields. Concise syntheses of biologically intriguing kinetin and potent kinase inhibitor olomoucin were thus achieved in just one and two steps, respectively.