4-pyrimidone derivatives

Details 4-pyrimidone derivatives 4-pyrimidone derivatives

C - Chemistry, Metallurgy

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C07D 239/47 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01)

Patent

CA 1140129

ABSTRACT 11732 A process is disclosed for preparing compounds of formula (1) :- Image (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 Image (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.

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