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Synthesis of 5‐(2,3‐ditritiopropoxy)‐3‐(1,2,5,6‐tetrahydropyrid‐4‐yl)indole ([ 3 H]CP‐96,501): A selective ligand for the serotonin (5‐HT 1B ) receptor
Author(s) -
Macor John E.,
Burkhart Carol A.,
Lebel Lorraine A.,
Koe B. Kenneth,
Chalabi Phillip M.,
Windels James C.,
Roth Robert W.
Publication year - 1991
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.2580290302
Subject(s) - chemistry , indole test , serotonin , radioligand , ligand (biochemistry) , stereochemistry , 5 ht receptor , chemical synthesis , receptor , in vitro , biochemistry
The synthesis of [ 3 H]CP‐96,501 [5‐(2,3‐ditritiopropoxy)‐3‐(1,2,5,6‐tetrahydropyrid‐4‐yl)indole], a selective radioligand for the serotonin (5‐HT 1B ) receptor and analog of RU‐24,969, is described. 5‐Hydroxyindole is converted in two steps to 5‐(2‐propenyloxy)‐3‐(N‐ t ‐butoxycarbonyl‐1,2,5,6‐tetrahydropyrid‐4‐yl)indole ( 3 ). Hydrogena‐tion or tritiation of 3 followed by removal of the t ‐butoxycarbonyl protecting group afforded CP‐96,501 ( 1a ) and [ 3 H] CP‐96,501 ( 1b ), respectively.