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Synthesis of carbon‐14 labeled CI‐926 and CI‐927, new antihypertensives
Author(s) -
Hays Sheryl J.
Publication year - 1987
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.2580240402
Subject(s) - chemistry , ethylene oxide , carbon 14 , ethylene , dilution , carbon fibers , medicinal chemistry , radiochemistry , carbon atom , organic chemistry , ring (chemistry) , catalysis , physics , materials science , composite material , quantum mechanics , composite number , copolymer , thermodynamics , polymer
3‐[4‐]4‐(3‐Methylphenyl)‐1‐piperazinyl[butyl]‐2,4‐imidazolinedione, CI‐926 ( 1 ), and 3‐[4‐4‐(3‐ethoxyphenyl)‐1‐piperazinyl]butylamino‐5,5‐dimethyl‐2‐cyclohexen‐1‐one, CI‐927 ( 2 ) are new antihypertensive agents which have been carbon‐14 labeled in three steps starting from ethylene‐ 14 C 2 oxide ( 5 ). The overall radiochemical yields for 1 and 2 were 69% and 66% respectively. The specific activity for both compounds was initially 22.6 mCi/mmol before final dilution.