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    • 9. 发明授权
    • 2-Ketoalkyl-4(3H)-quinazolinones
    • 2-酮基烷基-4(3H) - 喹唑啉酮
    • US4183931A
    • 1980-01-15
    • US831446
    • 1977-09-08
    • James F. WolfeTerry L. Rathman
    • James F. WolfeTerry L. Rathman
    • C07D239/90A61K31/505C07D239/91
    • C07D239/90
    • 2-Ketoalkyl-4(3H)-quinazolinones of the formula ##STR1## wherein R.sub.1 is an aliphatic, cycloaliphatic or hydrocarbon aromatic group of 1-10 carbon atoms;A is divalent alkylene of 1 to 10 carbon atoms;R.sub.2 is an aliphatic, cycloaliphatic, hydrocarbon aromatic or heterocyclic group of 1-10 carbon atoms formed by condensing an acyl ester of the formula R.sub.2 COOR' which can be dissociated to form --COR.sub.2 and R'OH in which R' is the alcoholic portion of said ester; andR.sub.3 and R.sub.4 are each hydrogen, hydroxy, amino, halogen, trifluoromethyl, alkyl, alkoxy, alkylthio or alkylsulfonyl each of 1-4 carbon atoms, the substituents other than hydrogen when present being preferably in the 6- and/or 7-position of the quinazolinone nucleusprovide compounds having useful activity as CNS depressants and anticonvulsants. A process is provided for preparing such compounds by ester condensation of a corresponding 2-alkyl-3-substituted-4(3H) quinazolinone with a condensable ester and excess sodium hydride in the presence of a strong ionization solvent such as refluxing 1,2-dimethoxyethane.
    • 具有式“IMAGE”的2-酮基烷基-4(3H) - 喹唑啉酮,其中R 1是1-10个碳原子的脂族,脂环族或烃芳族基团; A是1至10个碳原子的二价亚烷基; R2是通过将可分解形成-COR 2和R'OH的式R 2 COOR'的酰基酯缩合形成的1-10个碳原子的脂族,脂环族烃芳族或杂环基团,其中R'是醇的部分 所述酯; 并且R 3和R 4各自为1-4个碳原子的氢,羟基,氨基,卤素,三氟甲基,烷基,烷氧基,烷硫基或烷基磺酰基,当存在时除氢之外的取代基优选为6-和/或7-位 喹唑啉酮核提供具有CNS抑制剂和抗惊厥药有用活性的化合物。 提供了一种通过在强电离溶剂如1,2-二氯乙烷的回流溶剂存在下,通过相应的2-烷基-3-取代-4(3H)喹唑啉酮与可冷凝的酯和过量的氢化钠的酯缩合来制备此类化合物的方法, 二甲氧基乙烷。