An example of diastereoselective and enantioselective synthesis of thiochroman derivatives through a sulfa-Michael-Michael cascade sequence is disclosed. This is a significant complement of the quinine-thiourea catalyzed sulfa-Michael-Michael cascade reaction. The densely functionalized target thiochromans were obtained in high diastereoselectivities, and with high to excellent enantioselectivi...

2-Amino-4-phenyl-5,6,7,8-tetrahydroquinoline-3-carbonitrile (3) was synthesized by treating cyclohexanone (1) with 2-benzylidenemalononitrile (2) in the presence of ammonium acetate. The reactivity of compound 3 towards dimethylformamide dimethyl acetal (DMF-DMA), carbon disulfide, urea, thiourea, formamide, formic acid, acetyl chloride and isothiocyanate were studied. In addition, the antimicr...

Normal coordinate analysis of urea, thiourea and selenourea was performed on the basis of the general valence force field; Wilson's FG matrix method has been used. The final force fields were obtained through an iterative selfconsistent method. The vibrational assignment for these molecules is discussed. Calculated mean amplitudes of vibration for the urea series and their deuterated derivative...

The organocatalytic Michael addition of malonates to symmetric unsaturated 1,4-diketones catalyzed by thiourea and squaramide derivatives with Cinchona alkaloids afforded the formation of a new C-C bond in high yields (up to 98%) and enantiomeric purities (up to 93%). The absolute configuration of the product was suggested from comparison of the experimental and calculated VCD spectra of the re...

Dehydrogenative desulfurization of thiourea derivatives (RNHC(S)NHR') has been achieved, to give carbodiimides (RN=C=NR'), in the reaction with hydrosilane and (η(5)-C5H5)Fe(CO)2Me. The obtained carbodiimide reacted with (η(5)-C5H5)Fe(CO)(SiR3) formed in the reaction to give an N-silylated η(2)-amidino iron complex, which was isolated and then characterized by X-ray analysis.

α-Enone 1, reacts with hydrazines, hydroxylamine hydrochloride, thiourea, diethylmalonate, malononitrile ethyl cyanoacetate to give the corresponding indazole, oxime, isoxazole, quinazoline, chromene and quinoline derivatives. The structures of all the synthesized compounds were confirmed by micro analytical and spectral data. The antimicrobial and the antitumor activities of some of the synthe...

A simple and efficient approach towards one step synthesis of 6-amino-5-cyano-4-phenyl-2-mercapto pyrimidine and its hydroxyl derivatives have been developed by three component condensation of aromatic aldehydes, malononitrile and thiourea/urea in presence of phosphorus pentoxide (Scheme 1).

In search of bioactive molecules in the class of functionally substituted heterocyclic compounds, we synthesized some new N-(1-methyl-1H-pyrazole-4-carbonyl)thiourea derivatives and evaluated their analgesic and sedative effects. The obtained compounds were characterized by elemental analysis, IR and NMR spectroscopic analyses and evaluated for their analgesic and sedative effects.

A series of thiourea derivatives (7-23, 25-27) of 1-aminotetrahydronaphthalene (4) and 1-amino-2-hydroxytetrahydronaphthalene (5) were synthesized in single pot in 48-90% yield and evaluated for their anorexigenic activity. Among them compounds 10, 14, 15, 16 and 22 exhibited significant anorexigenic activity without any antidepressant effect and provided a new structural lead for appetite supp...

An asymmetric Friedel-Crafts alkylation reaction of 2-furfuryl ketones with β-trifluoromethyl enones has been developed via formal trienamine catalysis of a bifunctional primary amine-thiourea substance derived from L-tert-leucine, delivering the furan derivatives incorporating a stereogenic trifluoromethyl (CF3) group in good to high yields with excellent enantioselectivity.