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Synthesis of N-(2-chloro-5-methylthiophenyl)- N′-(3-methyl-thiophenyl)- N′-[3H3]methylguanidine, {[3H3]CNS-5161}

✍ Scribed by Andrew R. Gibbs; Hiromi Morimoto; Henry F. VanBrocklin; Philip G. Williams; Anat Biegon


Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
89 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis


The preparation of the title compound, [ 3 H 3 ]CNS-5161, was accomplished in three steps starting with the production of [ 3 H 3 ]iodomethane (CT 3 I). The intermediate N-[ 3 H 3 ]methyl-3-(thiomethylphenyl)cyanamide was prepared in 77% yield by the addition of CT 3 I to 3-(thiomethylphenyl)cyanamide, previously treated with sodium hydride. Reaction of this tritiated intermediate with 2-chloro-5-thiomethylaniline hydrochloride formed the guanidine compound [ 3 H 3 ]CNS-5161. Purification by HPLC gave the desired labeled product in an overall yield of 9% with >96% radiochemical purity and a final specific activity of 66 Ci mmol À1 .


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