Synthesis of Carbon-14 Analogue of 1,5 Diaryl-5-~14C-l,2,3-triazoline and Triazoles

摘要

Introduction:1,5 diaryl-1,2,3-txiazoline and triazoles frequently exhibit anticonvulsant properties and compare favorably with prototype antiepileptic drugs. The presence of the methylsulphone group at the para-position of one of the phenyl rings in analogues compounds, has let to compounds with good anti-inflammatory properties and cyclooxyganase enzyme inhibitor potency. To further elucidate the mechanism of action and to support the on-going metabolism studies4 the need arose to synthesize the corresponding carbon-14 compounds, with the label situated in a biologically stable site. The desired products, were synthesized according to the synthetic pathway shown in following Scheme.