| 摘要 |
<p>The invention relates to partly new 3-(1H^_-tetrazol-5-yl)-4H^_-pyrido[1,2-a^_]pyrimidin-4-ones of general formula (I) and pharmaceutically acceptable salts and/or hydrates and the preparation thereof. These compounds possess significant antiallergic or antiulcer activity. The subjects of our invention are compounds of general formula (I) and pharmaceutically acceptable salts and/or hydrates thereof, wherein R stands for hydrogenatom, C1-4 alkyl group, or C6-10 aryl group; R1 stands for hydrogenatom, C¿1-4? alkyl group, halogenatom, hydroxyl group, nitro group, carboxyl group, C2-5 alkoxycarbonyl group or C7-12 aralkoxy group; R?2¿ represents hydrogenatom, C¿1-4? alkyl group, or halogenatom; and a process for the preparation thereof. The invention also relates to a process for the preparation of compounds of general formula (I) and pharmaceutically acceptable salts and/or hydrates thereof, which comprises cyclising a 3-(2-pyridylamino)-2-(1H^_-tetrazol-5-yl)acrylnitrile of general formula (II), (wherein the meanings of R, R?1 and R2¿ are the same as defined above) in acidic media and converting the compound of general formula (I) thus obtained into a pharmaceutically acceptable salt thereof or, if desired, liberating the base from its salt, or converting it into another salt thereof in a way known per se.</p> |
