Synthesis of unlabelled, 3H- and 125I-labelled β-CIT and its ϖ-fluoroalkyl analogues β-CIT-FE and β-CIT-FP, including synthesis of precursors

The full synthesis of the cocaine congener 2β-carbomethoxy-3β-(4-iodophenyl)tropane (β-CIT) and its N-fluoroalkyl analogues, fluoroethyl- and fluoropropyl-nor-β-CIT (β-CIT-FE and β-CIT-FP) starting from cocaine is described. The synthetic routes include the preparation of precursors for labelling with radionuclides such as 11C, 18F, 76Br, 123I, 125I and 3H. Here we also report the labelling with 125I or 3H for use in autoradiographic examination of human brain sections.