Nycomed Amersham Plc

Amersham International Plc

Bp Chemicals Limited

Amersham Plc

Jonathan R Dilworth

Colin M Archer

Ian A Latham

Russell M Thompson

Panna Jobanputra

John Glenn Sunley

Michael James Baker

James D Kelly

Kwok W Chiu

David V Griffiths

Nigel Wheatley

Cores for technetium radiopharmaceuticals

.sup.99m Tc complexes of formula L.sub.n Tc.dbd.NR, L.sub.n Tc--N.dbd.NY, or L.sub.n Tc--(N.dbd.NY).sub.2 wherein each L is independently a monodentate or multidentate ligand;

A synth .sup.99m Tc complex which contains the moiety Tc.dbd.NR, Tc--N.dbd.NY or Tc(--N.dbd.NY).sub.2 and an organic ligand which confers biological target-seeking properties on the technetium complex, where R is an aryl group, a substituted or unsubstituted alkyl group or the group --NR.sup.1 R.sup.2 ; Y is an aryl group or a substituted or unsubstituted alkyl group; and R.sup.1 and R.sup.2 are H, aryl groups or substituted or unsubstituted aliphatic or cyclic alkyl groups, and are the same or different provided that both are not hydrogen. Radiopharmaceuticals comprising this complex are also described, together with methods for the preparation of the complex.

Novel complexes of technetium (.sup.99 Tc or .sup.99m Tc) which contain the moiety Tc.dbd.NR, Tc--N.dbd.NY or Tc(--N.dbd.NY).sub.2, and a ligand which confers biological target-seeking properties on the complex, wherein R represents an aryl group, a substituted or unsubstituted alkyl group, or the grouping .dbd.NR.sup.1 R.sup.2 ; Y represents an aryl group or a substituted or unsubstituted alkyl group; and R.sup.1 and R.sup.2 are hydrogen, aryl groups or substituted or unsubstituted aliphatic or cyclic alkyl groups, and may be both the same or different, provided that both are not hydrogen. The complexes are suitable for use in radiopharmaceuticals for a variety of clinical applications. Methods for the preparation of these technetium complexes are also described.

A process or the liquid phase carbonylation of methanol or a reactive derivative thereof comprises contacting carbon monoxide with a liquid reaction composition comprising methanol or a reactive derivative thereof, a halogen promoter and a rhodium catalyst system comprising a rhodium component and a bidentate phosphorus-sulphur ligand, the ligand comprising a phosphorus dative center linked to a sulphur dative or anionic center by a substantially unreactive backbone structure comprising two connecting carbon atoms or a connecting carbon and a connecting phosphorus atom. Novel rhodium ligand complexes of formula [Rh(CO)L].sub.m and Rh(CO)LY] wherein Y is a halogen, m is a number less than 10 and L is ##STR1## wherein the R groups are independently selected from C.sub.1 to C.sub.20 alkyl, cycloalkyl, aryl, substituted aryl and optionally substituted aralkyl; the R.sup.5 groups are selected from hydrogen, C.sub.1 to C.sub.20 alkyl, cycloalkyl, aryl, substituted aryl, aryl and optionally substituted aralkyl groups; the R.sup.1 to R.sup.4 groups are independently selected from hydrogen, C.sub.1 to C.sub.20 alkyl and optionally substituted aralkyl; X is a non-coordinating substitutent such as C.sub.1 to C.sub.20 alkyl, cycloalkyl, aryl, substituted aryl, C.sub.1 to C.sub.20 alkoxy, C.sub.1 to C.sub.20 alkylthio, trialkylsilyl or triarylsilyl, preferably, Si(CH.sub.3).sub.3 or methyl and n is 0 to 4 preferably 0 or 1.

Process for the carbonylation of methanol or a reactive derivative

Tridentate mono-anionic ligands have the structure

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Essex, United Kingdom

Jonathan R Dilworth