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Synthese d'un Derive du Methomyl Marque au 14 C avec une Photoaffinite Potentielle Pour le Site Recepteur des Mitochondries Texas
Author(s) -
Aranda G.,
Herbert M.,
Pichat L.
Publication year - 1986
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.2580230304
Subject(s) - chemistry , acetic acid , medicinal chemistry , yield (engineering) , reagent , bromide , azide , hydrogen bromide , nuclear chemistry , stereochemistry , organic chemistry , bromine , materials science , metallurgy
SYNTHESIS OF A LABELLED DERIVATIVE OF METHOMYL WITH POTENTIAL AFFINITY FOR THE BIOLOGICAL ACTIVE SITE OF MITOCHONDRIAS TEXAS The Grignard reagent from 1‐chloro‐4‐methoxy butane was carbonated with 14 CO 2 giving [carboxyl 14 C]‐5‐methoxy pentanoic acid Yield: 80%. Specfic activity : 24,3 mCi/mmole Treated with dry hydrogen bromide in acetic acid, the latter gave [carboxyl 14 C]‐5‐bromopentanoic. acid with was condesed with diphenylphosphoryl azide leading to 5‐bromobutyl [carbonyl 14 C] isocyanatc. Without isolation, the latter was reacted with methylthioacetoxy giving [carbonyl 14 C) S‐methyl‐N [(4‐azidobutyl. carbamoyl) oxy] thivacetimidate with an overall yield of 15,7 %/ 14 CO 2 and a radiochemical purity of 99,8 %. Specific activity : 23,7 mCi/mmole.