4-PYRIMIDONE DERIVATIVES

摘要

11732 A process is disclosed for preparing compounds of formula (1) : (1) and acid addition salts thereof where Het is an optionally substituted 5- or 6- membered fully unsaturated nitrogen containing heterocyclic group where the substituents (which can be the same or different) are one or more C1-4 alkyl, trifluoromethyl, halogen, hydroxy, C1-4 alkoxy or amino groups; n is 2 or 3; Z is hydrogen or C1-4 alkyl; A is C1-5 alkylene optionally interrupted with oxygen or sulphur and B is hydrogen, methyl, C3-6 cycloalkyl, an optionally substituted heteroaryl group where the substituents (which can be the same or different) are one or more C1-4 alkyl, C1-4 alkoxy or hydroxy groups; or B is a naphthyl, 5- or 6-(2,3-dihydro-1,4-benzodioxinyl) or a 4- or 5-(1,3-benzodioxolyl) group or an optionally substituted phenyl group where the substituents (which can be the same or different) are one or more C1-4 alkyl, C1-4 alkoxy, halogen, aryl-(C1-4 alkoxy), hydroxy, C1-4 alkoxy-C1-4 alkoxy, trifluoromethyl, di(C1-4 alkyl) amino, phenoxy, halophenyl, or C1-4 alkoxyphenyl groups which comprises reacting a compound of formula (4) : Het-CH2L (4) or an acid addition salt thereof where Het is as defined with reference to formula (1) provided that any substituents which interfere with the reaction are protected and L is a group displacable with thiol with a compound of formula (3):11732 (5) or an acid addition salt thereof where n, Z, A and B are as defined with reference to formula (1) provided that any phenolic hydroxy groups within B are optionally protected, and thereafter removing any protecting groups.