Radioiodination of 4-benzyl-1-(3-iodobenzylsulfonyl)piperidine, 4-(3-iodobenzyl)-1-(benzylsulfonyl)piperazine and their derivatives via isotopic and non-isotopic exchange reactions

摘要

A mild and simple technique for preparing of 4-benzyl-1-(3-[I-125]iodobenzylsulfonyl)piperidine, 4-(3-[I-125]iodobenzyl)-1-(benzylsulfonyl)piperazine and their derivatives, as sigma-1 receptor ligands, with relatively high radiochemical yields via nucleophilic substitution reaction by means of isotopic and non-isotopic exchange reactions is described. Some factors affecting the radiochemical yield were commonly studied in presence of acidic medium at elevated temperature. Unfortunately, the radiochemical yields were weak. Some attempts were carried out in presence of polar aprotic solvents to enhance the radiochemical yield. N,N-Dimethylformamide was proved highly efficient for preparing of radioiodinated 4-benzyl-1-(3-iodobenzylsulfonyl)piperidine (4-B-[I-125]-IBSP, 70 +/- A 5.7 %) and 4-(3-iodobenzyl)-1-(benzylsulfonyl)piperazine (4-[I-125]-IBBSPz, 72 +/- A 6.0 %) at moderate temperature (100-105 A degrees C) within 8 h. The specific activities of 4-B-[I-125]-IBSP and 4-[I-125]-IBBSPz (6,534.2 and 5,927.4 MBq/mmol) were obtained respectively.