Radioiodination and bioevaluation of nitrofurantoin for urinary tract imaging

Nitrofurantoin (NF) was labeled with iodine‐125 via electrophilic substitution reaction. Some factors affecting the radiochemical yield of ¹²⁵I‐NF, such as NF concentration, chloramine‐T (CAT) concentration, pH of the reaction mixture, reaction time, temperature, and reaction medium, were studied. The maximum yield of ¹²⁵I‐NF (90%) was obtained by using 3.7 MBq of Na¹²⁵I, 1 mM CAT, 1 mM NF in DMF, at pH 2 and 60 °C within 5 min. The specific activity of ¹²⁵I‐NF reaches 33.3 MBq/0.2 mmol, and the ¹²⁵I‐NF was completely separated and purified by means of high pressure liquid chromatography. The biological distribution in normal mice indicates the suitability of radioiodinated NF for urinary tract imaging. Copyright © 2012 John Wiley & Sons, Ltd.     

Synthesis of a 35S‐labeled dinucleoside phosphorothioate prodrug,an orally bioavailable anti‐HBV agent

The ³⁵S‐labeled, dinucleoside phosphorothioate 1, an orally available agent against hepatitis B virus, was prepared in eight steps with high specific activity and radiochemical purity. Radiolabeled 3H‐benzodithiole‐3‐one‐1,1‐dioxide was synthesized in four steps from ³⁵S₈ and was used as the sulfurizing reagent. Copyright © 2012 John Wiley & Sons, Ltd.