Novel Quinazolinones and Their Use in the Preparation of Triazoloquinazolinone Derivatives

摘要

Novel quinazolinone derivatives of general formula II, IMAGE (wherein X represents a hydrogen or halogen atom or a nitro, trifluoromethyl, methyl or methoxy radical; n is 2, 3, 4 or 5; and R1 and R2, which may be the same or different, each represents a hydrogen atom or a C1-5 alkyl or C1-5 hydroxyalkyl radical or, together with the nitrogen atom to which they are attached, they represent a saturated heterocyclic ring optionally containing a further heteroatom and/or optionally being substituted by one or more substituents selected from hydroxy, C1-5 alkyl, C1-5 hydroxyalkyl, C3-6 cycloalkyl, formyl, C1-5 acyl, C2-6 alkoxycarbonyl and aryl radicals (said aryl radicals themselves being optionally substituted by a halogen atom or a trifluoromethyl radical), with the proviso that any -NH- groups in -NR1R2 are in protected form, are useful in a process for the preparation of compounds of formula I, IMAGE by reacting the compound of formula II with a formylating agent followed, if required by removal of any protecting groups and/or reaction with an acid to form a salt.