[~(18)F]fluoromethylbenzylsulfonate ester: a rapid and efficient synthetic method for the N-[~(18)F]fluoromethylbenzylation of amides and amines

摘要

We have prepared 4-[~(18)F]fluoromethylbenzylsulfonate esters as fluoromethylbenzylating agents. These agents are readily prepared by an [~(18)F]fluoride ion displacement of the corresponding bissulfonate esters. The application of these 4-[~(18)F]fluoromethylbenzylsulfonate esters to N-alkylation reaction of spiperone and 1-phenylpiperazine shows that the products 3-N-(4-[~(18)F]fluoromethylbenzyl)spiperone and l-N-(4-[~(18)F]fluoromethylbenzyl)-4-phenylpiperazine are rapidly produced with high radiochemical yields under a no-carrier-added condition.