1,4,7,10-tetraazacyclododecane-butyltriol, its gadolinium complex, pharmaceutic and diagnostic drug containing that, preparation of the compound, and preparation of pharmaceutic

1991 
PURPOSE: To provide a new compd. useful as a diagnostic agent for NMR, X-ray, ultrasonic and radiation diagnosis and as a radiotherapeutic drug. CONSTITUTION: The compd. is expressed by formula I. In the formula I, R 1 is H, metal ion equiv.; R 2 is butyltriol. The compd. is, for example, 10-(2,3,4- trihydroxybutyl)-1,4,7-trixcarboxymethyl-1,4,7,10-tetraazacyclododecane. The compd. of formula I is obtd. by allowing a compd. expressed by formula II to react with a substrate into which the group R 2 as protected is introduced, delblocking and isolating -NH- groups, alkylating with an acetic acid deriv. expressed by HalCH 2 COOY (Hal is Cl, Br, I), and then removing the protecting groups. In the formula II, X is N protecting group, -CH 2 COOY-; Y is H, ammonium cation, alkali metal, protecting group. COPYRIGHT: (C)1993,JPO
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