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The synthesis of a range of new phosphine-containing polydentate ligands has been achieved by addition of sulfur and nitrogen nucleophiles to dimethylvinylphosphine sulfide, followed by reduction of the resulting phosphine sulfides with lithium aluminium hydride.

A strategy used to develop several potential 99mTc-based myocardial imaging agents is described. Ether-substituted 1,2- and 1,3-diphosphine ligands were prepared and used to produce a range of cationic Tc-99m complexes for subsequent screening. Ligand/core combinations were optimised in several cases to produce agents showing good heart uptake and retention in both animals and humans. A range of phosphine-containing polydentate ligands has also been prepared and their potential for use in myocardial imaging agents assessed. A tridentate phosphine/amine/thiolate chelate system has been developed which gives a [99mTc(PNS)2]+ complex showing good heart uptake in the rat. Synthetic routes to ether-substituted derivatives of this PNS ligand system have also been developed.

A synthesis of 2-amino-1-hydroxyethylene-1,1-bisphosphonic acid 3 has been developed from N -phthaloylglycine via dimethyl 2-( N -phthaloylamino)acetylphosphonate 1 . The preparation of the N -methylated and N , N -dimethylated derivatives 4 and 5 has been achieved by the reaction of 3 with formic acid and formaldehyde. The synthesis of 1-amino-2-hydroxyethylene-1,1-bisphosphonic acid 9 (RR′H) and its N -methylated and N , N -dimethylated analogues has been achieved by the reaction of phosphorus trichloride and phosphorous acid with the appropriate O -benzyl protected hydroxyacetamide, followed by catalytic hydrogenolysis of the protecting group.

A synthesis of 2-amino-1-hydroxyethylene-1,1-bisphosphonic acid 3 has been developed from N -phthaloylglycine via dimethyl 2-( N -phthaloylamino)acetylphosphonate 1 . The preparation of the N -methylated and N , N -dimethylated derivatives 4 and 5 has been achieved by the reaction of 3 with formic acid and formaldehyde. The synthesis of 1-amino-2-hydroxyethylene-1,1-bisphosphonic acid 9 (RR′H) and its N -methylated and N , N -dimethylated analogues has been achieved by the reaction of phosphorus trichloride and phosphorous acid with the appropriate O -benzyl protected hydroxyacetamide, followed by catalytic hydrogenolysis of the protecting group.

A strategy used to develop several potential 99mTc-based myocardial imaging agents is described. Ether-substituted 1,2- and 1,3-diphosphine ligands were prepared and used to produce a range of cationic Tc-99m complexes for subsequent screening. Ligand/core combinations were optimised in several cases to produce agents showing good heart uptake and retention in both animals and humans. A range of phosphine-containing polydentate ligands has also been prepared and their potential for use in myocardial imaging agents assessed. A tridentate phosphine/amine/thiolate chelate system has been developed which gives a [99mTc(PNS)2]+ complex showing good heart uptake in the rat. Synthetic routes to ether-substituted derivatives of this PNS ligand system have also been developed.

The N-1:N-3 protonation ratio in mono-protonated 2,4-diaminopyrimidine has been determined from 3JC-2,H-6 by using the N-1- and N-3-methylpyrimidinium iodides as model systems.