Verfahren zur Herstellung von neuen Chinazolon-Verbindungen
The invention comprises compounds of the formula n which R1 represents a hydrogen atom or a C1- 4 alkyl, phenyl or phenyl-C1- 2 alkyl group, R2 and R3, which may be the same or different each represent a hydrogen atom or a saturated or unsaturated aliphatic hydrocarbon group, or R2 and R3, togethe...
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| Zusammenfassung: | The invention comprises compounds of the formula n which R1 represents a hydrogen atom or a C1- 4 alkyl, phenyl or phenyl-C1- 2 alkyl group, R2 and R3, which may be the same or different each represent a hydrogen atom or a saturated or unsaturated aliphatic hydrocarbon group, or R2 and R3, together with the adjacent nitrogen atom, form a heterocylic ring which may contain a further hereto atom, R4 represents a chlorine or bromine atom or a C1- 4 alkoxy group in the 6- or 7-position, and n is an integer from 1 to 3; and physiologically tolerable, acid-addition salts thereof. The compounds are prepared by (a) subjecting a compound of the formula to an intramolecular condensation at an elevated temperature and, if R1 is hydrogen and, if desired, alkylating or arylating the compound obtained; or (b) reacting an anthranilic acid of the formula or a reactive derivative thereof, for example an ester, with an amide of the formula or an amide ester of the formula in which R5 represents a C1- 2 alkyl group, or with a correspondingly substituted nitrile or amidine of a basically substituted carbonic acid, at an elevated temperature, and if desired, alkylating or arylating the compound obtained at the amide nitrogen atom; or (c) condensing a compound of Formula III or a reactive derivative thereof, for example an ester, with a halogeno-alkyl-imide acid ester of the formula VI in which hal represents a halogen atom, to form an o - halogeno - alkyl - quinazolone of the formula and reacting this compound with an amine of the formula and, if desired, alkylating or arylating the compound thus obtained at the amide nitrogen atom. Starting materials of the Formula II are prepared by reacting a 2-(o-chloracylamino)-benzoic acid amide of the formula with an amine of the formula Pharmaceutical compositions having analgesic and sedative action comprise a compound of the invention or a physiologically tolerable acid-addition salt thereof, together with a pharmaceutically suitable carrier. |
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