Following to the computational expectation, our previously reported intriguing 1,3-proton shift of 4,4,4-trifluorobut-2-yn-1-ols was successfully extended to the 4,4,4-trifluorobut-2-en-1-ol system under metal-free conditions to afford the corresponding saturated ketones in high to excellent chemical yields using such a convenient and easy-to-handle base as DBU at the toluene refluxing temperat...

In the presence of strong bases (NaH, DBU, KOH), ethyl 4-chloromethyl-6-methyl-2-oxo1,2,3,4-tetrahydropyrimidine-5-carboxylate and 4-mesyloxymethyl-6-methyl-5-tosyl-1,2,3,4tetrahydropyrimidin-2-one are transformed into novel tricyclic compounds, diethyl 9-methyl-5methylene-3,11-dioxo-2,3,4,5,6a,7,10,11-octahydro-1,6-methano[1,3]diazepino[1,7-e][1,3,5]triazocine-6,8(1H)-dicarboxylate and 9-methy...

[reaction: see text] 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 ...

Objective(s) 7-prenyloxycoumarins including 7-isopentenyloxycoumarin, auraptene and umbelliprenin, and herniarin have been widely recognized as bioactive coumarins. This paper presents the ways to synthesis these compounds. Materials and Methods 7-prenyloxycoumarins were synthesized by reaction between 7-hydroxycoumarin (' M) and relevant prenyl bromides (1.5 M) in acetone at room temperatur...

objective(s) 7-prenyloxycoumarins including 7-isopentenyloxycoumarin, auraptene and umbelliprenin, and herniarin have been widely recognized as bioactive coumarins. this paper presents the ways to synthesis these compounds. materials and methods 7-prenyloxycoumarins were synthesized by reaction between 7-hydroxycoumarin (' m) and relevant prenyl bromides (1.5 m) in acetone at room temperat...

In three earlier papers, the structures and biological potencies of numerous mono- and dicyclic antagonists of GnRH were reported. Among these, two families, each containing two to four members were identified that had very high antagonist potencies in an antiovulatory assay (within a factor of 2 of those of the most potent linear analogues) and high affinities (K(i) < 0.5 nM) for the rat GnRH ...

The amidine bases DBU (1,8-diazabicyclo[5.4.0]undec-7-ene) and DBN (1,5-diazabicyclo[4.3.0]non-5-ene) display nucleophilic behaviour towards highly electrophilic p-nitrophenyl carbonate derivatives with ring opening of the bicyclic ring to form corresponding substituted ε-caprolactam and γ-lactam derived carbamates. This simple method presents a unified strategy to synthesize structurally diver...