METHODS FOR PREPARING 4,6-DISUBSTITUTED 2-ISOCYANATOPYRIMIDINES AND THEIR USING AS INTERMEDIATE SUBSTANCES FOR SYNTHESIS OF BIOLOGICALLY ACTIVE COMPOUNDS Russian patent published in 2004 - IPC

FIELD: organic chemistry, chemical technology. SUBSTANCE: invention relates to the improved method for preparing compounds of the formula (I) wherein each residue X and Y means independently of one another hydrogen, halogen atom, (C₁-C₄)-alkyl, (C₁-C₄)-alkoxy-group or (C₁-C₄)-alkylthio- group being each among three latter residues is unsubstituted or substituted with one or some residues among the group including halogen atom, (C₁-C₄)-alkoxy-group or (C₁-C₄)-alkylthio- group or means di-[(C₁-C₄)-alkyl] -amino-group, (C₃-C₆)-cycloalkyl, (C₃-C₅)-alkenyl, (C₃-C₅)-alkynyl, (C₃-C₅)-alkenyloxy-group or (C₃-C₅)-alkynyloxy- group wherein compound of the formula (II) or its salts wherein X and Y have values indicated in the formula (I) are subjected for interaction with 1-6 moles of phosgene per 1 mole of compound of the formula (II) in the presence of 2-3.5 mole equivalents of organic amino-base per mole of compound of the formula (II) and in the presence of aprotonic organic solvent at reaction temperature in the range from 30 C to +60 C. Invention relates also to the improved method for preparing compounds of the formula (III) by interaction of corresponding compounds of the formula (I) with nucleophilic compound of the formula A-Q. Proposed methods provide the simplification of process and to enhance total yields and/or purity of end compounds. EFFECT: improved preparing methods. 11 cl, 7 ex