Synthesis of novel 3,4‐diaryl‐1H‐pyrroles

The synthesis of a series of novel 3,4‐diaryl‐1H‐pyrroles and related arylalkenes from p‐bromo thiophenol, tosylmethyl isocyanide and commercially available materials is reported. Arylalkenes having electron‐withdrawing substituents gave higher yield of 3,4‐diaryl‐1H‐pyrroles.     

Efficient synthesis of 6‐aryl‐2‐chloronicotinic acids via pd catalyzed regioselective suzuki coupling of 2,6‐dichloronicotinic acid

A regioselective Suzuki coupling of 2,6‐dichloronicotinic acid with aryl boronic acids to synthesize 6‐aryl‐2‐chloronicotinic acids is described. Regioselectivity was achieved in aqueous dioxane using the routinely used catalyst Pd(PPh₃)₄.     

Phenacylsulfonylacetic acid methyl ester‐synthon for 1,2,3‐selena/thiadiazoles and 2H‐diazaphospholes

A new class of 1,2,3‐selena/thiadiazoles and 2H‐diazaphospholes were synthesized by exploiting α‐ketomethylene group in phenacylsulfonylacetic acid methyl ester.     

One‐pot synthesis of symmetrically disubstituted 3H‐phenoxazin‐3‐ones by selective oxidative condensation with LTA

A one‐pot synthesis of some new 2,8‐disubstituted 3H‐phenoxazin‐3‐ones from 4‐substituted‐2‐aminophenols through a selective oxidative condensation by lead tetraacetate in acetic acid is described.     

Synthesis,structure and investigations of tuberculosis inhibition activities of new 4‐methyl‐1‐substituted‐1H‐1,2,4‐triazole‐5(4H)‐thione

By the reaction aminomethylation, chloromethylation and acylation of 4‐methyl‐4H‐1,2,4‐triazole‐3‐thiol, 4‐methyl‐1‐substituted‐1H‐1,2,4‐triazole‐5(4H)‐thione 1‐8 were obtained. Molecular structure of the obtained compounds was confirmed by an elemental analysis, IR, ¹H NMR and ¹³C NMR spectra and additionally by X‐ray analysis for 2. Six new compounds 1,2,4‐7 were tested for antibacterial activity against Mycobacterium smegmatis, Mycobacterium phlei and avirulent strain Mycobacterium H₃₇Ra.     

A general and versatile synthesis of 3‐phenylthio β‐lactams as lead molecules for 3‐methyl‐2‐azetidinones

Ketene‐imine cycloaddition using phosphorus oxychloride and benzenesulfonyl chloride under the described reaction conditions yielded trans 3‐phenylthio 2‐azetidinones in good yields. Desulfurization using Raney nickel and alkylation finally afforded trans 3‐methyl‐2‐azetidinones in a stereoselective manner.     

1,3‐Dibromo‐5,5‐dimethylhydantoin (DBH) as an efficient promoter for acetylation of 3‐arylsydnones in the presence of acetic anhydride under neutral conditions

1,3‐Dibromo‐5,5‐dimethylhydantoin (DBH) has been found to efficiently promote the conversion of various 3‐arylsydnones to their 4‐acetyl congeners in the presence of acetic anhydride under neutral conditions in satisfactory yields.     

Application of the acetate of baylis‐hillman adducts of salicylaldehydes in the synthesis of methyl 2‐oxo‐2,3‐dihydrobenzo[b]oxepine‐4‐carboxylates

A simple synthesis of several methyl 2‐oxo‐2,3‐dihydrobenzo[b]oxepine‐4‐carboxylates from Baylis‐Hillman adducts of O‐benzyl protected 2‐hydroxybenzadehydes has been described through the acetylation, cyanation, debenzylation, as well as acid assisted Pinner cyclization.     

Synthesis and antimicrobial activity of some new N‐(substituted phenyl)‐N′‐[2,3‐dihydro‐2‐oxido‐3‐(4′‐fluorophenyl)‐1H‐(1,3,2)benzoxazaphosphorin 2‐yl]ureas

Substituted benzoxazaphosphorin 2‐yl ureas were synthesized by reacting 2‐(4‐fluoro‐phenylamino)‐methylphenol (4) with different carbamidophosphoric acid dichlorides (3) in the presence of triethylamine in dry toluene at 45‐50 °C and characterized by spectral data. These compounds were found to possess good antimicrobial activity.