Premium
Synthesis of carbon‐14 labelled indolic 5HT 1 receptor agonists
Author(s) -
Waterhouse Ian,
Cable Karl M,
Fellows Ian,
Wipperman Mark D,
Sutherland Derek R
Publication year - 1996
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/(sici)1099-1344(199611)38:11<1021::aid-jlcr921>3.0.co;2-o
Subject(s) - chemistry , cyanation , indole test , tryptamines , ring (chemistry) , cleavage (geology) , organic chemistry , carbon fibers , stereochemistry , combinatorial chemistry , medicinal chemistry , catalysis , biochemistry , tryptamine , materials science , geotechnical engineering , fracture (geology) , composite number , engineering , composite material
Syntheses of carbon‐14 labelled versions of indolic 5HT 1 agonists sumatriptan (GR43175) (1a), GR40370 (2a) and naratriptan (GR85548) (3a) are described. Introduction of the label via cyanation of ketoformanilides, formed by oxidative cleavage of an indole ring, ensured incorporation of carbon‐14 at the metabolically stable C‐2 position of the indole.