ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

A short, multigram synthetic route to methyl 2-amino-4-methyl-3-thiophenecarboxylate as a precursor for preparation of new biologically active derivatives and novel materials

R. Pavlovicova, J. Minarikova, D. Hudecova, and D. Vegh

Abstract: A multigram method of preparation of methyl 2-amino-4-methyl-3-thiophenecarboxylate is described. The acid ester and its derivatives are the key intermediates for the synthesis of novel ethylenic thiophenes and of fused thiophenes as Histamine H-2 receptor antagonists with gastric antisecretory activity. The antimicrobial effects of these compounds have been tested on various strains of bacteria, yeasts, and filamentous fungi. The highest antimicrobial activity was found with derivative IIa on filamentous fungi Botrytis cinerea and Fusarium moniliforme (IC50 = 25 mu g cm(-3) and 80 mu g cm(-3), respectively).

Chemical Papers 51 (6B) 437–442 (1997)