Benzylpyrimidine derivative



(57)【要約】 (修正有) 【目的】 ベンジルピリミジン誘導体及びそのそれを用 いた医薬品化合物の製造法が提供される。 【構成】 一般式(III)で表わされる利尿活性を有す る化合物及びそれらを合成する際の重要中間体である一 般式(VIII)及び一般式(IX)で表わされるベンジルピ リミジン誘導体。 〔式中、R 4 ,R 4a は水素またはC 1−4 アルキルで あり、R 5 及びR 6 はハロゲン、C 1−4 アルキル、ま たはC 1−4 アルコキシである〕
PURPOSE: To obtain the subject novel compound showing antibacterial activity and diuresis, and to provide a synthesis method using the above compound as an intermediate. CONSTITUTION: This compound is the one shown by formula I (R 4 is H or a 1-4C alkyl; R 5 and R 6 are each a halogen, 1-4C alkyl or 1-4C alkoxy) or its acid additon salt or the one shown by formula II or its acid additon salt, or the one shown by formula V (R 4a is H or a 1-4C alkyl), obtained by reacting (A) a compound shown by formula III (R 7 and R 8 are each a 1-4C alkyl or the like) with (B) a compound shown by formula IV (R 9 is H, hydroxy, a 1-4C alkylthio or mercapto). The compound shown by formula V can be also obtained by amination of the compound shown by formula I or II. COPYRIGHT: (C)1996,JPO




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