The preparation of 1,3,4-oxadiazoles from 1,2-diacylhydrazines using XtalFluor-E ([Et(2)NSF(2)]BF(4)) as cyclodehydration reagent is described. Various functionalized 1,3,4-oxadiazoles were synthesized and it was found that the use of acetic acid as an additive generally improved the yields.

In this study a series ofnew1-(2-aryl-5-phenethyl-1,3,4-oxadiazol-3(2H)-yl)ethanones 2a-e was synthesized by the cyclization of imines 1a-e using acetic anhydride. The products were evaluated for anti-bacterial and anti-fungal activity. Among the newly synthesized compounds, 1-(2-(4-(dimethylamino)phenyl)-5-phenethyl-1,3,4-oxadiazol-3(2H)-yl)ethanone (2a)and1-(2-(4-chlorophenyl)-5-phenethyl-1,3...

Rapid and highly efficient synthesis of 2- or 2,5-substituted 1,3,4-oxadiazoles by the condensation of aryl carboxylic acid hydrazides and orthoesters can be achieved under microwave irradiation using an unmodified commercial over in unsealed vessels.

A new series of 5-(indole-2-yl)-3-substituted 1,2,4-oxadiazoles were synthesized and evaluated for their anticancer activities. Structures of the compounds were confirmed by spectroscopic methods. Structural modifications were done to improve the antiproliferative activity of compound 1. The results indicated that a benzyloxyl substituent on the C-4 position was better than a methyl substituent...

α-Imino gold carbenoid species have been recognized as key intermediates in a plethora of processes involving gold-activated alkynes. Here, we explored the pathways Au(I)-catalyzed [3 + 2] reaction between mild nucleophiles: anthranil, 1,2,4-oxadiazole, or 4,5-dihydro-1,2,4-oxadiazole, and an ynamide, PhC≡C-N(Ts)Me, proceeding via formation aforementioned α-imino carbene intermediate which, aft...

Many organic sulfones have been shown to possess antibacterial, antimalarial, anthelmintic, antilepral, antineoplastic, anti-inflammatory and antidiabetic acitivities. These sulfones are commonly prepared from sodium benzenesulfinate 1-0 which plays an important role in organic synthesis. However the application of 1-0 in solid-phase synthesis has received relatively less attention. This projec...