A microwave-assisted, one-pot, two-step protocol was developed for the construction of polysubstituted 2-aminoimidazoles. This process involves the sequential formation of imidazo[1,2-a]pyrimidinium salts from readily available 2-aminopyrimidines and alpha-bromocarbonyl compounds, followed by opening of the pyrimidine ring with hydrazine. [reaction: see text]

Environmentally friendly synthetic methods were developed for the selective preparation of new 2,3-dihydro-1,4-thiaselenine derivatives in high yields based on reactions 2-bromomethyl-1,3-thiaselenole with alcohols and water at room temperature. The reaction was accompanied by a rearrangement ring extension, leading to six-membered heterocyclic compounds, family 2-organyloxy-2,3-dihydro-1,4-thi...

In the title compound, C(22)H(15)Cl(2)NO, the terminal chloro-benzene rings are oriented at 44.51 (15) and 86.06 (17)° with respect to the central polysubstituted benzene ring, and make a dihedral angle of 49.48 (17)°with each other. In the crystal, mol-ecules are linked by weak C-H⋯O and C-H⋯N inter-actions.

A novel exo-selective [6+3] cycloaddition approach for the highly enantioselective synthesis of polysubstituted piperidines was developed. The developed methodology was applied in a one-pot [6+3]-[4+2] dicycloaddition, allowing the construction of structurally and stereochemically rich polycyclic compounds from simple building blocks.

A novel and convenient approach to the synthesis of polysubstituted isochromanones is described. Irradiation of 2-formyl phenylalkeno-derivatives with UV light in benzene solution afforded the corresponding products in up to 98% yield. The possible reaction mechanism is proposed and further supported by the isotopic experiments.

A facile and efficient one-pot synthesis of polysubstituted pyridin-2(1H)-ones from readily available enaminones and the cyanomethyl sulfonium bromide salt in the presence of cesium carbonate is developed, and a mechanism involving sequential nucleophilic vinylic substitution (S(N)V), intramolecular nucleophilic cyclization and dealkylation reactions is proposed.

The biliary excretion and blood/plasma ratios of four novel 5-bromo-6-alkoxy- 5,6-dihydro prodrugs to S-ethyl-2'-deoxyuridine (EDU) including (-)-trans-(5S, 6S)-S-bromo-S-ethyl-6-methoxy-S, 6-dihydro-2'-deoxyuridine (BMEDU), (+ )-trans( SR, 6R)-S-bromo-S-ethyl-6-ethoxy-S, 6-deoxyuridine (BEEDU), (+ )-trans-(SR, 6R)-5-bromo-5-ethyl-6-ethoxy -S, 6-dihydro-S '-O-valeryl-2 ':.deoxyuridine (VBE...

A novel protocol to synthesize multisubstituted benzo[b][1,4]oxazepines from N-(2-haloaryl)enaminones has been developed. In this procedure, only 2 equiv. of Cs2CO3 was required. A variety of polysubstituted benzo[b][1,4]oxazepine derivatives were provided in up to 95% yield for 27 examples.