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Synthesis of 5‐ethyl‐2‐{5‐[4‐(2‐hydroxyethyl)piperazin‐1‐ylsulfonyl]‐2‐ n ‐propoxyphenyl}‐7‐ n ‐propyl‐3,5‐dihydro‐4 H ‐pyrrolo[3,2‐ d ]‐[2‐ 14 C]pyrimidin‐4‐one·2 HCl ( 14 C‐SK3530·2 HCl)
Author(s) -
Shin HyunIl,
Lee Juyoung,
Kim DaeKee
Publication year - 2006
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.1116
Subject(s) - chemistry , yield (engineering) , sequence (biology) , medicinal chemistry , nuclear chemistry , stereochemistry , metallurgy , biochemistry , materials science
A new 14 C‐labelled PDE5 inhibitor, 5‐ethyl‐2‐{5‐[4‐(2‐hydroxyethyl)piperazin‐1‐ylsulfonyl]‐2‐ n ‐propoxyphenyl}‐7‐ n ‐propyl‐3,5‐dihydro‐4 H ‐pyrrolo[3,2‐ d ]‐[2‐ 14 C]pyrimidin‐4‐one·2 HCl ( 14 C‐SK3530·2 HCl) ( 1· 2 HCl) was synthesized through a straightforward six‐step sequence from the readily available [ 14 C‐carbonyl]methyl salicylate ( 2 ). The overall radiochemical yield of the 1· 2 HCl from 2 was 10.5%, and its radiochemical purity was 98.8%. Copyright © 2006 John Wiley & Sons, Ltd.
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