Richard J. Seguin

Synthesis of [Ring‐3H] Dopamine and Fluoro Analogues at High Specific Activity

Abstract Dopamine and several fluoro analogues were labeled with tritium at high specific activity by a catalytic tritium dehalogenation of polybromo precursors.

Tritiation and characterization of several biologically active nightshade alkaloids

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

Dopamine: approaches to its side chain labeling with tritium.

Methods are presented to tritiate the side chain of dopamine.

High specific activity tritium labelling of some sigma-1 receptor agonists

The high specific activity tritiation of (+)-SKF-10,047 (1) and N,N-dimethyltryptamine (4) is described. [N-allyl-3H] (+)-SKF-10,047 (3) was prepared by Lindlar catalyst tritiation of (+)-N-propargylnormetazocine (2) and [N-methyl-3H] N,N-dimethyltryptamine (6) was synthesized by the alkylation of N-methyltryptamine (5) with [3H] methyl iodide. Both sigma-1 synthetic agonist 3 and endogenous agonist 6 have been useful in studying this receptor.

Synthesis of [15, 16-3H] beta-funaltrexamine

Beta-funaltrexamine is a unique irreversible antagonist for the mu-opiate receptor and would be useful as a tritiated radioligand. Starting from high specific activity [15, 16-³H] naltrexone, [15, 16-³H] beta-funaltrexamine was synthesized and characterized by means of a two-step reductive amination-acylation process.