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Synthesis of [ 3 H]CP‐93,129: A selective radioligand for the 5‐HT 1B receptor
Author(s) -
Macor John E,
Ryan Kevin,
Chalabi Phillip M.,
Windels James C.,
Roth Robert W.
Publication year - 1990
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.2580281109
Subject(s) - chemistry , radioligand , agonist , tritium , pyridine , 5 ht receptor , halogenation , chemical synthesis , stereochemistry , bicyclic molecule , receptor , radioligand assay , serotonin , medicinal chemistry , organic chemistry , biochemistry , in vitro , physics , nuclear physics
The synthesis of [ 3 H]‐CP‐93,129, a potent radioligand for the serotonin 5‐HT 1B receptor, is described. 5‐Butoxypyrrolo[3,2‐b]pyridine ( 2 ) is converted in 3 steps to 5‐butoxy‐1‐phenylsulfonyl‐2‐tritiopyrrolo[3,2‐b]pyridine ( 3c ) via lithiation of C2, iodination of that anion, and tritium reduction. ( 3c ) is converted to the title compound in two more steps analogous to methodology used in the synthesis of CP‐93,129, a potent and selective 5‐HT 1B agonist.