PROCESS FOR PRODUCING 2,4-DIAMINO-6-PYPERIDINOPYRIMIDINE-3-OXY (ITS MODIFICATIONS)
A process for the preparation of 6-piperidino-2,4-diaminopyrimidine- 3-oxide of the formula (I> comprises reacting 6-hydroxy- 2,4-diaminopyrimidine of the formula (II). with either (a) a sulfonyl halide of the general formula (V> R-SO2-hal (V> wherein R stands for a C1-4 alkyl group or a ph...
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Zusammenfassung: | A process for the preparation of 6-piperidino-2,4-diaminopyrimidine- 3-oxide of the formula (I> comprises reacting 6-hydroxy- 2,4-diaminopyrimidine of the formula (II). with either (a) a sulfonyl halide of the general formula (V> R-SO2-hal (V> wherein R stands for a C1-4 alkyl group or a phenyl group optionally having up to three C1-4 alkyl substituents and hal represents halogen, treating the resulting novel sulfonate of the general formula (III), wherein R is as defined above, with an oxidizing agent in an aprotic solvent, reacting, the resulting novel N-oxide of the general formula (IV), wherein R is as defined above, directly with piperidine, or first acylating it with a carbonyl halide of the general formula (XI), R'CO-hal (XI> wherein R' represents a C1-4 alkyl group or a phenyl group optionally substituted with a halogen substituent and hal stands for halogen, and reacting the resulting compound of the general formula (IX), wherein R and R' are as defined above, with piperidine; or b) a sulfonyl halide of the general formula (V), wherein R and hal are as defined above, reacting the resulting sulfonate of the general formula (III), wherein R is as defined above, in an aprotic solvent with a peracid of the general formula (X), R'-COOOH (X> wherein R' is as defined above, and reacting the resulting compound of the general formula (IX), wherein and R' are as defined above, with R piperidine. |
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