PURPOSE: To obtain the subject novel chelate forming compd. which is useful as an in vivo diagnostic agent and a medicament for tumor treatment and has a reducing property and tissue specificity.
CONSTITUTION: A compd. of formula I [X is O, S, etc.; Y, Z are each OH, NHR3 (R3 is H, a 1 to 8C alkyl), etc.; U is H, carboxyl, etc.; (n) is 2 to 6; (m) is 2, 3; R1 exists only when (m) is two and H, benzyl, etc.], its technetium complex, its rhenium complex and its salt, for example, tris-(3(2,3 dihydroxyphenoxy) propyl) amine hydrochloride. This compd. is obtd. by bringing an amine of formula II (Nu is a nucleus dissociation group such as Cl, Br; R1 is a substituent R1) into reaction with an arom. compd. of formula III (U' is U which protects hydroxy or carboxy; Y', Z' are Y, Z or their precursor or protecting X, Y) for about 6 hours to 6 days at 50 to 200°C in a polar solvent under a base catalyst, then generating the desired substituents Y and Z in the product and further, subjecting the product to complex formation with a technetium isotope.
Kramp, Dr. Wolfgang
Neumeier, Dr. Reinhard
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