Process for purification of 9-(2,6- dihalobenzyl)adenines

Details Process for purification of 9-(2,6- dihalobenzyl)adenines Process for purification of 9-(2,6- dihalobenzyl)adenines

C - Chemistry, Metallurgy

07

D

260/242.3

C07D 473/34 (2006.01)

Patent

CA 1111423

ABSTRACT OF THE INVENTION 9-(2,6-Dihalobenzyl)adenines substantially free of the 3-isomer, useful as coccidiostats, are prepared in a number of ways. One is by alkylating a salt of adenine with 2,6-dihalobenzyl halides in a two phase system in the presence of a phase transfer catalyst and then treating the resulting mixture of positional isomers, containing primarily the desired 9-isomer contaminated by substantial amounts of the mutagenic 3-isomer, by selectively dealkylating the 3-isomer with sulfuric acid in the presence of a carbenium ion trap to obtain the 9-isomer substantially free of the 3-isomer. Alternatively, 9-(2,6-dihalobenzyl)adenines are directly prepared uncontaminated with positional isomers from 4,5,6-triaminopyrimidine via 7-(N-formyl-N-dihalo- benzylamino)[l,2,5]thiadiazolo[3,4-d]pyrimidine.

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