METHOD FOR PREPARING SULFONULAMINOPYRIMIDINE COMPOUNDS (VARIANTS), INTERMEDIATE SUBSTANCES AND METHODS FOR THEIR PREPARING Russian patent published in 2007 - IPC C07D239/42 C07D239/22 C07D239/34 

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to novel methods (variants) for synthesis of 2-(N-methyl-N-methanesulfonylamino)-pyrimidine of the formula (3) and aminopyrimidine compound of the formula (8) that can be used in synthesis of the known medicinal preparation - rosuvastatin. In compounds of formulae (3) and (8) R represents lower alkyl; each of R¹ and R² represents independently hydrogen atom, alkyl group, alkylsulfonyl group or arylsulfonyl group. Method for synthesis of compound of the formula (3) involves the following steps: (I) isobutyrylacetate ester of compound of the formula (5): wherein R represents lower alkyl is subjected for interaction with 4-fluorobenzaldehyde and urea in the presence of proton compound and metal salt; (II) compound synthesized in reaction at step (I) is oxidized; (III) obtained product after oxidation from stage (II) is subjected for interaction with organic sulfonyl halide of the formula (2): R'-SO₂-X wherein R' represents lower alkyl substituted possibly with halogen atoms, phenyl substituted possibly with 1-3 groups chosen from nitro-group, halogen atoms, branched or direct lower alkyl, lower alkoxy-group; X represents halogen atom or organic sulfonic anhydride of the formula (2a): (R'-SO₂)-O wherein R' has a value given above in the presence of a base; (IV) product of reaction at step (III) is subjected for interaction with N-methyl-N-methanesulfonamide in the presence of a base. Method for synthesis of compound of the formula (8) involves a step for interaction of corresponding 2-halide- or 2-substituted sulfonylpyrimidine with corresponding amino-compound. Also, invention relates to novel intermediate compounds and methods for their synthesis. Proposed methods provide avoiding toxic compounds and to obtain compounds of high purity and with the high yield.

EFFECT: improved methods of synthesis.

35 cl, 27 ex