Spiperone: Tritium labelling at high specific activity.

An efficient method is described to tritiate spiperone at high specific activity.

Tritium labelling of several potent fluorinated antipsychotic drugs at high specific activity.

Methods are presented to synthesize and characterize [methylene-3H] haloperidol 2 and [N-methyl-3H]trifluoperazine 6.

Tritiation of imipramine and pseudo irreversible analogues 3-cyanoimipramine and 2-nitroimipramine at high specific activity.

Methods are presented to synthesize and characterize [N-methyl-3H] imipramine 3, [N-methyl-3H] 3-cyanoimipramine 6 and [N-methyl-3H] 2-nitroimipramine 9.

The synthesis and characterization of [2,3-3H] gamma-aminobutyric acid via 4-aminotetrolic acid at high specific activity.

Gamma-aminobutyric acid was labelled with tritium by the tritium gas catalytic reduction of a convenient 4-aminotetrolic acid derivative. The purified product was characterized by HPLC and tritium NMR.

Tritium labelling and characterization of the antimalarial drug (+/-)-chloroquine by several methods.

To study its mechanism of antimalarial action, a tritium labelled analogue of (+/-)-chloroquine was required at high specific activity. Two synthetic methods were successfully employed. [3-3H] (+/-)-Chloroquine 2 was prepared by the catalytic tritium dehalogenation of an iodo precursor and [N-ethyl-3H] (+/-)-chloroquine 4 was synthesized by the alkylation of (+/-)-desethylchloroquine with [3H] ethyl iodide.