A simple and economic synthesis of 3,4-dihydropyrimidin-2(1H)-ones using ammonium trifluoroacetate as catalyst and as solid support is accomplished. Easy workup procedure for the synthesis of title compounds is well arrived at and is well documented.

In 1893, P. Biginelli reported the synthesis of functionalized 3, 4-dihydropyrimidin-2(1H)-ones (DHPMs) via three-component condensation reaction of an aromatic aldehyde, urea, and ethyl acetoacetate. In the past decade, this long-neglected multicomponent reaction has experienced a remarkable revival, mainly due to the interesting pharmacological properties associated with this dihydropyrimidin...

Mammalian flavin-containing monooxygenase (FMO) is active towards many drugs with a heteroatom having the properties of a soft nucleophile. Thiocarbamides and thiones are S-oxygenated to the sulfenic acid which can either react with glutathione and initiate a redox-cycle or be oxygenated a second time to the unstable sulfinic acid. In this study, we utilized LC-MS/MS to demonstrate that the oxy...

Reactions of 2-chloro-4-fluoropyridine (8), 2-chloro-4-nitropyridine (9), and their corresponding N-oxides 7 and 3 with the n-heptanolate anion were investigated in three solvents. The desired 2-chloro-4-heptyloxypyridine-N-oxide (4a) was obtained most efficiently from 3 in DMSO. A reaction of 4a with AcSNa followed by deacetylation with MeONa gave the sodium salt of 4-heptyloxy-1-hydroxypyridi...