Fused quinazolinones and a process for production thereof

Details Fused quinazolinones and a process for production thereof Fused quinazolinones and a process for production thereof

1974-11-07

1976-09-14

Thomas, Jr., James O.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

260251A, C07D26500, C07D27300, C07D29500

Patent

active

039806456

ABSTRACT:
Fused quinazolinone derivatives of the formula, ##SPC1##
Wherein R.sub.1 and R.sub.2 are individually hydrogen, C.sub.1.sub.-4 alkyl, C.sub.1.sub.-4 alkoxy, nitro, C.sub.1.sub.-4 alkylsulfonyl or halogen; R.sub.3 is pyridyl, thienyl or a group of the formula ##SPC2##
Wherein R.sub. 4 is hydrogen or halogen; R is hydrogen, C.sub.1.sub.-4 alkyl, C.sub.2.sub.-5 alkenyl, aralkyl, (C.sub.3.sub.-6 cycloalkyl)C.sub.1.sub.-4 alkyl, (C.sub.1.sub.-4 alkoxy)C.sub.1.sub.-4 alkyl, (C.sub.1.sub.-4 alkylthio)C.sub.1.sub.-4 alkyl, hydroxy-C.sub.1.sub.-4 alkyl or C.sub.2.sub.-5 alkanoyloxy-C.sub.1.sub.-4 alkyl; Y is oxygen, or a group of the formula N - R.sub.5, wherein R.sub.5 is hydrogen or C.sub.1.sub.-4 alkyl; and Z is C.sub.2.sub.-5 alkylene or alkenylene, are prepared by reacting a trihaloacetamidophenyl ketone derivative of the formula, ##SPC3##
Wherein R.sub.1, R.sub.2, R.sub. 3 and R are as defined above; and X.sub.1, X.sub.2 and X.sub.3 are halogen, with an amine of the formula, HY - Z - NH.sub.2, wherein Y and Z are as defined above, or a salt thereof, in the presence of a solvent or a mixture thereof. They have remarkable pharmacological properties such as anti-inflammatory, analgesic and/or uricosuric activities.

REFERENCES:
patent: 3329679 (1967-07-01), Sulkowski et al.
Sato et al.-"Yakugaku Zasshi" 90(5) pp. 629-633 (1970)-Synthesis of Quinazolinone Derivatives.

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