Xiao-shu He, D. Matecka, K. Lee
1994
Citations
0
Influential Citations
5
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
[123I]tert-Butyl 8-iodo-5,6-dihydro-5-methyl-6-oxo-4H-imidazo [1,5-a][1,4]benzodiazepine 3-carboxylate ([123I]3), a high affinity and selective radioligand for the diazepam insensitive (DI) benzodiazepine receptor was synthesized in 2 steps from tert-butyl 8-bromo-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine 3-carboxylate (4). A key step in the synthesis of this potential SPECT imaging agent utilized (Ph3P)3Pd mediated stannylation of 4 with (Bu3Sn)2 to the corresponding 8-tributyltin derivative 5. Iododestannylation of 5 with no carrier added [123]NaI in aqueous ethanolic CH3CO3H furnished [123I]3 (85%) in greater than 98% radiochemical purity following TLC purification.