Preparation and Labeling of Thienopyrimidine and Environmental Remediation of by-products

Abstract

Thienopyrimidine was prepared using dehydrative cyclisation of phenylisothiocyanate with 4-aminopent-3-en-2-one (enaminone) in presence of dry acetone and Raioiodinated was performed using Chloramine–T and hydrogen peroxide methods as oxidizing agents. The conditions of radioiodination such as concentration of oxidizing agent, reaction time, concentration of thienopyrimidine and effect of pH were studied to get maximum yield. The optimum conditions for radioiodinations using chloramine–T method were 10µg Thienopyrimidine, 12 µg chloramine –T and 1 minute reaction time at pH 7.4. The optimum conditions for radioiodination using hydrogen peroxide method were 10µg  Thienopyrimidine, 10 µl hydrogen peroxide: acetic acid (1: 1) and 5 minutes reaction time at pH 7.4. In all cases, the by-products were removed using activated carbon to prevent the environmental threats.