Acta Pharm. 63 (2013) 409-418

 

full paper

Short communication

 

A convenient synthesis of new NSAID esters containing amino acid, urea and amide moieties

IVANA PERKOVIĆ, ZRINKA RAJIĆ DŽOLIĆ and BRANKA ZORC

bzorc@pharma.hr

University of Zagreb, Faculty of Pharmacy and Biochemistry, Zagreb, Croatia

Accepted March 12, 2013

 

A convenient synthetic method for the preparation of novel NSAID twin esters 6a-i containing amino acid residue, urea and amide moieties has been developed. The synthetic pathway applied for the preparation of target compounds and key intermediates 1-benzotriazolecarboxylic acid chloride (1), NSAID benzotriazolides 2a-c and N-(1-benzotriazolecarbonyl)-amino acids 3a-d involved benzotriazole as a synthetic auxiliary. The final preparation step of esters 6a-i included the solvent-free reaction of compounds 2a-c with amino acid derivatives 5a-g, bearing two hydroxyl groups, one at each terminal, beside urea and amide functionalities.

 

Keywords: NSAID, ester, amino acid, benzotriazole, urea, amide