B. Lingappa

Novel One‐Pot Synthesis of Aziridines Containing Sydnone Moiety

Abstract A novel series of 1,1a‐dihydro‐1‐aryl‐2‐(3‐aryl‐sydnone‐4‐yl)‐azirino[1,2‐a] quinoxalines were prepared in a one‐pot reaction of 2,3‐dibromo‐1‐(3‐arylsydnone‐4‐yl‐)‐3‐arylpropan‐1‐one with o‐phenylenediamine employing triethylamine in ethanol. The new compounds were well characterized by IR,1H NMR, mass spectra, and C,H,N analysis.

Synthesis and Biological Study of Some Novel 4-[5-(4,6-Disubstituted-2-thiomethylpyrimidyl)-4′-amino-1,2,4- triazol-3′-yl] thioacetyl-3-arylsydnones

A series of 4-[5-(4,6-disubstituted-2-thiomethyl pyrimidyl)-4′-amino-1,2-4-triazol-3′-yl]thioacetyl-3-arylsydnones 7a–i were synthesized by the reaction of 5-(4,6-disubstituted-2-thiomethylpyrimidyl)-4-amino-3-mercapto-1,2-4-triazoles 3 with 3-aryl-4-bromoacetyl sydnones 6 in an ethanol medium. The newly synthesized compounds 7a–i were screened for their antibacterial activity against E. coli and Serratia marcesens and for antibacterial activity against Aspergillus niger and Pencillium. Most of the tested compounds showed significant antifungal activity particularly against Pencillium at 10-μg/mL concentration comparable with that of the standard drug Flukanazole.

One-Pot Synthesis of Pyrimidinothiazolidinones and Their Anti-Inflammatory and Antimicrobial Studies

In the present investigation, we report a one-pot synthesis of the title compounds, 2-arylidene-5-(2,3,6-trimethyl-4-methoxyphenyl)-7-substituted-5H-pyrimidino-[2,3-b]thiazolidine-3-ones 6a–j and 2-(5-nitro-2-thienylidine)-5-(2,3,6-trimethyl-4-methoxyphenyl)-7-substituted-5H- pyrimidino-[2,3-b]thiazolidine-3-ones 7a–e. Thus, 6a–j and 7a–e were prepared in good yields by refluxing 4-(2,3,6-trimethyl-4-methoxyphenyl)-6-methyl/aryl-3,4-dihydropyrimidin-2-(1H)-thiones 5, monochloro acetic acid, and anhydrous sodium acetate with the appropriate aromatic aldehyde/5-nitro-2-thiophenediacetate in acetic acid/acetic anhydride medium. The structures of these new compounds were established on the basis of their analytical and spectral data. Some of the newly synthesized compounds were screened for their anti-inflammatory and antimicrobial activity. They show moderate anti-inflammatory activity, and some of them were found to be promising antibacterial and antifungal agents. Supplemental materials are available for this article. Go to the publishers online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.

4-(4-Bromo­phenyl­hydrazono)-1-(5-bromo­pyrimidin-2-yl)-3-methyl-2-pyrazolin-5-one

The asymmetric unit of the title compound, C14H10Br2N6O, contains two crystallographically independent molecules. The pyrazole ring of one molecule makes dihedral angles of 22.0 (3) and 3.5 (3)° with the pyrimidine and benzene rings, respectively; the corresponding values in the other molecule are 9.2 (3) and 2.1 (3)°, respectively. The molecules are linked by N—H⋯O, C—H⋯N and C—H⋯Br hydrogen bonds.