Dibra S.p.a.

Alessandro Scala

Giorgio Ripa

Carlo Felice Viscardi

Marcella Murru

Marina Ausonio

Maria Argese

Vittorio Valle

Emanuela Panetta

Patrizia Cossutta

Chiara Scotti

A process for the preparation of 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid and the salts thereof of formula (I) ##STR1## which comprises the following steps: a) carboxymethylation reaction of a suitable precursor in water, with a haloacetic acid,

Process for the preparation of

Process for the preparation of tetraazamacrocycles

A process for the preparation of tetraazamacrocycles of general formula (I) ##STR1## wherein n, p and q can independently be 0 or 1, comprising the following steps:

A process for the preparation of complexes of macrocyclic chelants with paramagnetic metal trivalent ions of formula (XII) ##STR1## wherein R.sub.1, R.sub.2 and Me.sup.3+ are as described in the following, comprising: a) reaction of 1,4,7,10-tetraazacyclododecane with triethyl orthoformate to give 5H,9bH-2a,4a,7,9a-octahydrotetraazacycloocta[cd]pentalene; b) carboxymethylation reaction in water; c) hydrolysis reaction in basic conditions; d) alkylation according to known methods with an epoxide in water; e) complexation according to known methods carried out in water by addition of a paramagnetic metal salt; f) purification by diafiltration, final desalting of the aqueous solution on ion exchange resins and g) crystallization or recovery.

Process for preparation of macrocyclic chelants and the chelates thereof

Process for the preparation of macrocyclic chelants and the chelates

A process for the preparation of tetraazamacro-cycles of general formula (I) ##STR1## wherein n, p and q can independently be 0 or 1, comprising the following steps:

A process for the preparation of complexes of macrocyclic chelants with paramagnetic metal trivalent ions of formula (XII) ##STR1## wherein R.sub.1, R.sub.2 and Me.sup.3+ are as described in the following, comprising: a) reaction of 1,4,7,10-tetraazacyclododecane with triethyl orthoformate to give 5H,9bH-2a,4a,7,9a-octahydrotetraazacycloocta�cd!pentalene; b) carboxymethylation reaction in water; c) hydrolysis reaction in basic conditions; d) alkylation according to known methods with an epoxide in water; e) complexation according to known methods carried out in water by addition of a paramagnetic metal salt; f) purification by diafiltration, final desalting of the aqueous solution on ion exchange resins and g) crystallization or recovery.

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Milan, Italy

Alessandro Scala