Patent ID: 7238338

Claim:
A method for synthesizing a radiohalogenated pyrimidine comprising, in order: i) dissolving a halogenated pyrimidine in a first solvent 1,4 dioxane at a temperature of between 40 and 60° C. to form an initial solution, the pyrimidine being selected from a group consisting of nucleosides, nucleotides, ribonucleosides, deoxyribonucleosides, 2′,3′ dideoxynucleosides and 5′ sugar-derivatized nucleosides and phosphonucleosides; ii) cooling the initial solution to a temperature of from 20 to 30° C. and adding bis(tributyltin) and triphenylphosphine palladium to the initial solution to produce a catalyzed solution; iii) heating the catalyzed solution under an inert atmosphere to a reaction temperature from 100 to 110° C. and for a reaction period of from 5 hours to 7 hours to produce an intermediate solution including a stannylated pyrimidine compound; iv) removing substantially all of the first solvent from the intermediate solution to obtain an intermediate composition, the intermediate composition including the stannylated pyrimidine compound; v) purifying the intermediate composition to produce a purified composition including the stannylated pyrimidine compound; vi) reacting the stannylated pyrimidine compound with a radiohalogen in a buffered reaction mixture at a pH from 5 to 8 to produce the radiohalogenated pyrimidine; vii) adding ascorbic acid to the reaction mixture; and viii) extracting the radiohalogenated pyrimidine from the reaction mixture to obtain a radiohalogenated pyrimidine for use as a diagnostic product.