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[6-chloro-3-pyridylmethyl-3H] neonicotinoids as high-affinity radioligands for the nicotinic acetylcholine receptor: Preparation using NaB3H4 and LiB3H4

✍ Scribed by Bachir Latli; Chit Than; Hiromi Morimoto; Philip G. Williams; John E. Casida

Publisher
John Wiley and Sons
Year
1996
Tongue
French
Weight
383 KB
Volume
38
Category
Article
ISSN
0022-2135

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✦ Synopsis

NaB'H, and LiB'H, at 78% and 97% isotopic enrichments, respectively, were used in the synthesis of 'H-labeled 1-(6-chloro-3-pyridyl)methyl-2-nitromethyleneimidazolidine (CH-IMI) and N'-[(6-chloro-3pyridyl) methyl1 -N"-cyano-N' -methylacetamidine (acetarniprid) (two very potent insecticides) and of 1-(6-chloro-3-pyridyl)methyl-2- iminoimidazolidine (desnitro-IMI) (a metabolite of the commercial insecticide imidacloprid) . 6-Chloronicotinoyl chloride was treated with either NaB'H, in methanol or LiE3H, in tetrahydrofuran and the resulting alcohol transformed to 2-chloro-5-chloromethylpyridine, which was then coupled to N-cyano-"-methylacetamidine to give

['HI acetamiprid (45 Ci/mmol) . 2-Chloro-5-chloro [3Hlmethylpyridine was also reacted with ethylenediamine and the product was either refluxed in absolute ethanol with 1,l-bis (methylthio) -2-nitroethylene to provide ['HICH-IMI or reacted in toluene with a solution of cyanogen bromide to produce ['Hldesnitro-IMI (each 5 5 Ci/mmol).

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