Process for the preparation of pyrimidyl-chinazolines

C - Chemistry – Metallurgy – 07 – D

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C07D 403/14 (2006.01) A61K 31/505 (2006.01) C07D 239/95 (2006.01) C07D 295/14 (2006.01) C07D 403/12 (2006.01)

Patent

CA 1156656

Process for the Preparation of Pyrimidyl-Quinazolines ABSTRACT OF THE DISCLOSURE Pyrimidyl-quinazolines having the general formula I Image (I) and pharmacologically acceptable acid addition salts thereof, wherein Rl and R2 denote hydrogen, alkyl having 1 to 6 C atoms, alkenyl having 2 to 6 C atoms cycloalkyl having 5 to 7 C atoms, phenyl or benzyl R3 denotes hydrogen, alkyl having 1 to 6 C atoms, alkenyl having 2 to 6 C atoms, phenyl, phen- alkyl having 1 to 4 C atoms in the alkyl radical, halogen, nitro, amino, alkylcarbonylamino having 1 to 6 C atoms in the aIkyl radical, phenyl- carbonylamino or formyl are prepared by a) reacting a compound of the formula II Image (II) wherein X denotes a mercapto radical or a halogen atom with a compound of the formula III Image (III) or b) reacting 2-piperazinyl-4-amino-6,7-dimethoxyquinazoline with a com- pound of the formula V Image wherein Hal denotes a halogen atom or c) introducing the substituent R3 into a compound of the formula VI Image in the 5-position of the pyrimidinedione nucleus and optionally converting the resulting compound of the formula I into an acid addition salt.

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