Substituted pyrimidin-2-ones, the salts thereof, processes...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/06 (2006.01) C07D 401/06 (2006.01) C07D 405/06 (2006.01) C07D 409/06 (2006.01) C07D 413/06 (2006.01)

Patent

CA 1159830

Abstract Compounds of the general formula:- Image 1 (wherein X represents a halogen atom or a trifluoromethyl group; R1 represents a hydrogen atom or a lower alkyl group and Het represents an optionally substituted C-attached 5-7 membered aromatic heterocyclic ring which ring contains one or more heteroatoms selected from O, N and S and optionally carries a fused ring) and where a basic group is present the salts thereof have been found to possess excellent metaphase arresting ability and are of use in combating abnormal cell proliferation Thus a knowledge of the cell division cycles of the normal and abnormal cells enables a cyctotoxic drug to be administered whilst the abnormal cells are in a phase susceptible to attack and whilst the normal cells are in a non-susceptible phase. The compounds of the invention are prepared by alkylation, deprotection of a protected keto group oxidation or electrophilic halogenation.

381682

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