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Synthesis of carbon-14 and tritium labeled dopamine beta-hydroxylase inhibitors of the imidazolinethione type

✍ Scribed by S. G. Senderoff; S. C. Shilcrat; S. H. Levinson; J. R. Heys

Publisher
John Wiley and Sons
Year
1989
Tongue
French
Weight
385 KB
Volume
27
Category
Article
ISSN
0022-2135

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✦ Synopsis

1 - [(3,

and 1 -[(3,5-difluorophenyI)methyl]-l,3-dihydro-2Himidazole-2-thione (SK&F 102048, SK&F 102055 and SK&F 102698, respectively) were synthesizyg in carbon-1 4 and tritium labeled forms Carbon-1 4 from potassium [ Clthiocyanate was incorporated into the imidazolethione ring of SK&F 102055 and SK&F 102698 at C-2 by c o n d e n s a t i o n w i t h N -( 2 , 2 -d i m e t h o x y e t h y I ) -3 , 5 -d i f l u o r o -4 -m e t h o x y b e n z e n e m e t h a n a m i n e o r N -( 2 , 2 -d i m e t hox y t h y I) -3,5d if I u or o be nz e n e m e t h ana m in e . Treat m Fp t of S K & F [2-C]102055 with boron tribromide gave SK&F 52-C]102048. Tritiated SK&F 102048 was synthesized by sodium [ Hlborohydride reduction of N-(3,5-difluoro-4-methoxyphenylmethylene)-2,2-dimethoxyethanamine, followed by condensation with potassium thiocyanate and dernethylation with boron tribromide.

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