2,3-dihydro-1H-pyrazoles were highly selectively synthesized via the Pd(0)-catalyzed coupling-cyclization reaction of 4-non-substituted 2-substituted 2,3-allenyl hydrazines with aryl iodides in moderate to good yields.

5-Hydroxy-3-oxopent-4-enoic acid esters can be efficiently transformed into the stable bis-potassium salts of the corresponding 5-hydroxy-3-oxopent-4-enoic acids, from which the sensitive acids are released in situ, the latter being converted into substituted 4-hydroxy-2H-pyran-2-ones, pyrazoles and isoxazoles under mild conditions; the efficiency of this method is demonstrated by the first syn...

A simple titanium complex catalyzes the coupling of alkynes, isonitriles, and monosubstituted hydrazines to generate substituted pyrazoles in a single step.

Non-fluorinated vinyldiazo compounds with trans-configuration irrespective of the nature of 3-R(1)-substituent (R(1) = H, Me, TBSO) even under ambient conditions easily cyclize to produce pyrazoles, while cis-stereoisomers undergo similar ring closure only at elevated temperatures or decompose to produce vinyloxocarbene reaction products. The 3-CF3-substituted analogues with cis- or trans-confi...

Ethyl diazoacetate (EDA), which is easily prepared from ethyl glycinate and NaNO2, reacts in situ with alkynes a water micelle environment without organic solvent to form pyrazoles. The reaction pH dependent, as the presence of protic catalysis (H2SO4 4 %, 3.5) mixture 3,5- 4,5-disubstituted pyrazoles was obtained, while, at 5.5, only 3,5-disubstituted isomer obtained. surfactant TPGS-750-M cru...

In vitro antimicrobial activity of seventeen heterocyclic nitrogen compounds {2-substituted pyrido [1,2-a] pyrimidin -4-oxo-1 [4]-3-Carbonitriles and ethyl 5-amino-3-(substituted) - pyrazole-3-Carboxylates} was tested against Escherichia coli, Bacillus subtilis and candida albicans strains, Antimicrobial activity was measured using standard two -fold serial dilution method and the minimum inhib...

The synthesis of trifluoromethyl-substituted pyridylboronic acids and pyrazolylboronic esters is described via lithiation-boronation protocols (Schemes 1, 3 and 4). A study of their palladium-catalysed cross-couplings with heteroaryl halides is presented. CF3-substituted aryl/heteroaryl-pyridines are thereby obtained (51-98% yields). Analogous cross-couplings have yielded heteroaryl-3-(trifluor...

A variety of heteroaromatic compounds, such as substituted pyridines, pyrazoles, indoles, 2-substituted imidazoles, 2-substituted imidazoles, 2-arylbenzazoles and pyrimidin-2(1H)-ones are synthesized by oxidative aromatization using the activated carbon and molecular oxygen system. Mechanistic study focused on the role of activated carbon in the synthesis of 2-arylbenzazoles is also discussed. ...