15891-46-0Relevant academic research and scientific papers
Reduction of the N-Propargyl Group with Tritium. General Procedure for the Preparation of N-3H>Allyl Opiate Ligands at High Specific Activity
Filer, Crist N.,Ahern, David G.,Fazio, Robert,Seguin, Richard J.
, p. 4968 - 4970 (1981)
Radiolabeled neurotransmitter receptor ligands are exceedingly valuable substances for obtaining information about their respective receptors, and a number of them possess the N-allyl group.A method is outlined to prepare (-)-N-(allyl)nalloxone (1b), (-)-N-(allyl)nalorphine (2b), and (+/-)-N-(allyl)normetazocine (3b) from their respective N-propargyl precursors.Triton nuclear magnetic resonance studies confirm labeling specificity.This labeling strategy affords the highest specific activities for such ligands reported to date and possesses a number of other advantages over previous methods.Utilization of such tritiated ligands for receptor binding assay will undoubtedly lead to a more comprehensive mapping of and increased information about their respective receptors.
