| 摘要 |
FIELD: organic chemistry, chemical technology, biochemistry, medicine. SUBSTANCE: invention proposes three alternative methods for preparing derivatives of pyrazolo[3,4-d] pyrimidine-7-one of the general formula (I) or their pharmaceutically acceptable salts wherein: Q represents oxygen atom; R1 represents hydrogen atom, lower alkyl, azetidinyl, -(C1-C6-alkyl)-Het wherein Het is taken among pyridyl, morpholinyl and piperidinyl, or (C1-C6-alkyl)-phenyl being azethidinyl, Het or phenyl in two latter groups can be substituted optionally with cyano-group, lower alkyl, CO2R7; R2 represents lower alkyl; R3 represents lower alkyl or cycloalkyl; R4 represents halogen atom, nitro-group, C(O)R8; R7 and R8 represent lower alkyl. The first method involves interaction of compound of the formula (II) wherein X represents removing group; R1, R2, R4 represent as they are given above with -OR3 generated from alcohol R3OH in the presence of a base or from solution of alcohol salt ZOR3 in suitable solvent wherein R3 means as given above; Z means cation of alkaline or alkaline-earth metal in the presence of trapping agent of the formula: TOC(O)W wherein OT represents OR3 or OT represents residue of volume alcohol or non-nucleophilic alcohol or residue of alcohol that can be removed by azeotropy method during reaction; C(O)W means residue of carboxylic acid. The second method involves interaction of compound of the formula (III) wherein X represents removing group; R1, R2, R4 mean such as they are given above with -OR3 generated as described above in the presence of above characterized trapping agent. The third method involves interaction of compound of the formula (V) wherein Q and R1-R4 have values given in the cl. 1 in the presence of a base taken among the group consisting of steric hindered base alkoxide, amide, hydride, oxide, carbonate or hydrocarbonate of alkaline or alkaline- earth metal and trapping agent characterized above. Invention provides preparing compounds of the formula (I) that are inhibitors of cyclic guanosine- -3',5'-monophosphate phosphodiesterase and useful, for example, in treatment of erectile dysfunction in males. EFFECT: improved preparing method, valuable medicinal properties of compounds, high yield. 7 cl, 3 tbl, 11 ex |
