Journal of labelled compounds and radiopharmaceuticals p. 115 - 122 (1997)
Update date:2022-08-02
Topics:
Lever, John R.
Johnson, Suzanne M.
Tritiated N1'-methyl and N1'-ethyl analogues of naltrindole (NTI) have been synthesized for evaluation as radioligands for studies of delta opioid receptors. The two N1'-alkyl-5',7'-dibromoNTI precursors for radiolabeling were prepared by base-promoted alkylation of 2,4-dibromophenylhydrazine with either iodomethane or iodoethane followed by condensation with naltrexone using the Fischer indole synthesis. Catalytic debromotritiation followed by HPLC purification afforded [3H]MeNTI (17.3 Ci/mmol) and [3H]EtNTI (22.5 Ci/mmol) with high chemical and radiochemical purities (≤ 99.8%).
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