Pyrimidine-2-sulphides and their s-oxides for use in medicine

Details Pyrimidine-2-sulphides and their s-oxides for use in medicine Pyrimidine-2-sulphides and their s-oxides for use in medicine

C - Chemistry, Metallurgy

07

D

260/260, 260/237

C07D 239/30 (2006.01) C07C 233/07 (2006.01) C07D 239/38 (2006.01) C07D 239/40 (2006.01) C07D 403/12 (2006.01) C07F 9/6512 (2006.01) C07H 17/02 (2006.01)

Patent

CA 1168240

ABSTRACT OF THE DISCLOSURE Compounds of the formula Image I (wherein X represents a halogen atom; n is 0, 1 or 2; R1 and R2, which may be the same or different, each represents a hydrogen atom. or a carboxyl, esterified carboxyl, amido or mono- or di-C1-4 alkylamido group or a C1-4 alkyl group which may if desired carry a carboxyl or esterified carboxyl group; and R3 represents a C1-32 saturated or unsaturated, straight or branched, cyclic or acyclic aliphatic group or an araliphatic or heterocyclic substituted aliphatic group, a hetero- cyclic group or an aryl group which groups may if desired carry one or more substituents selected from halogen atoms and oxo, nitro, hydroxy, etherified hydroxy, esterified hydroxy, primary, secondary or tertiary amino, acylamino etherified mercapto or S=O or -SO2 derivatives thereof and esterified phosphonic acid groups) and, where an acidic or basic group is present, physiologically compatible salts thereof have been found to be of use in combating abnormal cell proliferation. The compounds are prepared inter alia by oxidation of the corresponding sulfide, displacement of a leaving atom or group from the 2-position of the pyrimidine by reaction with a sulfinic acid or by ring closure of the pyrimidine ring.

368409

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