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Synthesis of Pyrazolo Linked Pyridine Carboxylic Acids and Evaluation of their Liquid Crystal and Biological Studies

Kallashettihally Rangappa Mahendra, Kuriya Madavu Lokanatha Rai

The present work deals with the synthesis and characterization of the pyrazole substituted pyridine carboxylate and carboxylic acid. The synthesized compounds are key intermediates for the synthesis of Apixaban. Apixaban is an anti-thromboembolic drug and also used as an anti-coagulating agent. Iodine substituted piperidine is the precursor material, it is treated with the chloroform and lactam to give substituted pyridine. The substituted pyridine is reaction with morpholine and the morpholine substituted compound is treated with an hydrazono acetate to give the piperidine carboxylate and limited hydrolysis to give pyridine carboxylic acids. The intermediate carboxylates and carboxylic acids are characterized for their biological and liquid crystal studies. The synthesized compounds have not showing any biological activity towards antibacterial and anti fungal assay. Further the final compounds showing very good activity towards the liquid crystalline studies. Carboxylic acid showing the very good liquid crystalline Properties. The synthesized compounds are analysed by 1H-NMR, 13C-NMR and LC-MS. The liquid crystal studies are characterized by Polarising optical microscopy and Differential scanning calorimetry.