Chlormadinone-4-14C acetate ( V ) was synthesized from 17%hydroxyprogesterone-4-14C ( I ) by dehydrogenation to the 4,6-diene ( I I ) which was converted to the 6-chloro-4,6-diene ( I V ) via the intermediate 6a,7aor-epoxy compound ( I I I ) , Acetylation of ( I V ) gave chIormadinone-4-14C acetate
Synthesis of N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidinium acetate [α-14C]
✍ Scribed by Maria Almeida; Arne Boman; Torbjörn Lundstedt
- Publisher
- John Wiley and Sons
- Year
- 2002
- Tongue
- French
- Weight
- 89 KB
- Volume
- 45
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.559
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✦ Synopsis
Abstract
^14^C‐Labelled N‐(2‐chloro‐3,4‐dimethoxybenzylideneamino)guanidinium acetate has been synthesized as a part of a four‐step procedure which involved decarboxylation of 2‐chloro‐3,4‐dimethoxybenzoic acid by Pb(OAc)~4~ to give 2‐chloro‐3,4‐dimethoxy‐1‐iodobenzene, followed by a selective lithiation at the iodine position and electrophilic substitution with N,N‐dimethylformamide [α‐^14^C] and final reaction with aminoguanidine bicarbonate. The specific activity was 59 mCi/mmol and the overall yield 49%. Copyright © 2002 John Wiley & Sons, Ltd.
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