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Synthesis of carbon-14 labeled CI-926 and CI-927, new antihypertensives

✍ Scribed by Sheryl J. Hays

Book ID
102374751
Publisher
John Wiley and Sons
Year
1987
Tongue
French
Weight
400 KB
Volume
24
Category
Article
ISSN
0022-2135

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✦ Synopsis

3-[4-~4-(3-Methylphenyl

)-1-piperazinyllbutyl]-2,4-imidazolinedione, CI-926 (11, and 3-[[4-4-(3-ethoxyphenyl)-l-piperazinyl] butyl lamino] -5,5-dimethyl-2-cyclohexen-l -one, CI-927 (2)

are new antihypertensive agents which have bee~~carbon-14 labeled in three steps starting from ethylene-C2 oxide ( 5 ) . The overall radiochemical yields for 1 and 2 were 69% and 66% respectively. initially 22.6 mCi/mmol before final dilution.

The specific activity for both compounds was

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## Abstract A reaction sequence suitable for the preparation of an analog of 2‐propyl‐1‐[2′‐(1H‐tetrazol‐5‐yl)[1,1′‐biphenyl]‐4‐yl]methyl‐4‐[2‐(trifluoroacetyl)‐1H‐pyrrol‐1‐yl]‐1H‐imidazole‐5‐carboxylic acid, with ^14^C at the methylene bridge was developed. The would‐be labeled fragment (12) was d