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Synthesis of tritium labelled (–)–U50,488, a selective kappa opioid agonist
Author(s) -
Thurkauf Andrew,
De Gosta Brian,
Rice Kenner C.
Publication year - 1989
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580270511
Subject(s) - chemistry , tritium , agonist , mandelic acid , kappa , combinatorial chemistry , chemical synthesis , resolution (logic) , stereochemistry , organic chemistry , receptor , in vitro , biochemistry , physics , linguistics , philosophy , artificial intelligence , computer science , nuclear physics
The preparation of 3 H labelled (‐)‐trans‐3,4‐dichloro‐N‐methyl‐N‐[2‐(1‐pyrrolidinyl) cyclohexyl]benzeneacetamide (U50,488) in four steps from N‐methylcyclohexylaziridine is described. The synthesis of the pharmacologically active (‐) isomer of U50,488 was accomplished through the resolution of the intermediate 2‐[1‐(3‐pyrrolinyl)]‐N‐methylcyclohexylamine using (+)‐mandelic acid.