Judith A. Egan

Biologically active equine estrogens and sulfate conjugates labelled with tritium at high specific activity.

Methods are presented to tritiate and characterize the steroid equilin as well as a structurally related 17-alpha alcohol metabolite and several 3-position sulfate conjugates.

The endogenous GABA analogue gamma-hydroxybutyric acid: Tritium labeling at high specific activity

Abstract2,3,4-3H] Gamma-hydroxybutyric acid (GHB, 4) was prepared by means of a catalytic tritium reduction of 2(5H)-furanone (2) followed by hydrolysis. It has proven useful as a tool to study the GHB receptor.

Tritium labeling of the local anesthetic tetracaine via a polyhalogenated precursor

Tetracaine was brominated to provide a convenient precursor employed in a catalytic tritiation yielding [3H] tetracaine.

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.

Tritium labelling and characterization of the cognition enhancing drug tacrine using several precursors

Tacrine and its analogues have shown promise as cognition enhancers and potential chemotherapeutic agents for Alzheimers disease. [3H]tacrine was required to explore its mechanism of action via receptor binding assay and the radioligand was prepared by means of catalytic dehalogenation of several brominated precursors.

Tritiation and characterization of several biologically active nightshade alkaloids

The tritiation of the nightshade alkaloids dihydrocapsaicin, atropine and nicotine is described.

Synthesis of some 6-keto morphinan mu opiate receptor agonists labelled with tritium at high specific activity

The high specific activity tritiation of oxymorphone and pentamorphone is described.

An Efficient Synthesis of the ACE Inhibitor [Phenyl‐3H] Lisinopril

Abstract An effective synthesis of [3H] lisinopril at high specific activity is described.

Potent antiviral agent WIN 54954: high specific activity labelling with tritium

Abstract Valuable antiviral compound WIN 54954 (2) was tritiated at high specific activity and the product was characterized.

Mirfentanil and A-4334: Tritiation at high specific activity

Methods are presented to synthesize and characterize [(3)H] mirfentanil and [(3)H] A-4334.