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    • 1. 发明公开
    • POLYAZACYCLOALKANE COMPOUNDS
    • 聚氮杂环烷烃化合物
    • EP0815091A1
    • 1998-01-07
    • EP96904204.0
    • 1996-03-01
    • NYCOMED IMAGING ASCOCKBAIN, Julian Roderick Michaelson
    • SCHULTZE, LisaBULLS, Alan, Ray
    • C07D257
    • C07D257/02
    • The present invention relates to tribenzylcyclen compounds of formula (I) (where R is hydrogen, or a C1-12 alkyl group optionally substituted by hydroxy, alkoxy or aryl groups or R is an amphiphilic aralkyl group comprising a N, S, O or P interrupted C2-25alkylene chain, e.g. a polyalkylene oxide chain or R provides a bridge to a second tribenzylcyclen group, but with the proviso that R is other than benzyl; X is CHR1, or where R is hydrogen two X groups may each represent CO groups; and R1 is hydrogen, a C1-6alkyl group optionally substituted by hydroxy, alkoxy or carboxy groups or an aralkyl group having 1 to 6 carbons in the alkyl moiety and optionally substituted in the aryl moiety by alkyl, alkoxy, hydroxy or isothiocyanate groups). These compounds are useful in the preparation of DO3A, N-substituted-1,4,7,10-tetraazacyclododecane-N',N',N'''-triacetic acids, and the phosphonic acid analogs.
    • 本发明涉及式(I)的三苄基环化合物(其中R为氢或任选被羟基,烷氧基或芳基取代的C 1-12烷基或R 2为包含N,S,O或P的两亲性芳烷基 中断的C2-25亚烷基链,例如聚亚烷基氧链或R提供桥接到第二个三苄基环庚基,但条件是R不是苄基; X是CHR1,或其中R是氢,两个X基团可各自代表CO基团 ;并且R 1为氢,任选被羟基,烷氧基或羧基取代的C 1-6烷基或在烷基部分具有1-6个碳原子并且在芳基部分任选被烷基,烷氧基,羟基或异硫氰酸酯基团取代的芳烷基) 。 这些化合物可用于制备DO3A,N-取代-1,4,7,10-四氮杂环十二烷-N',N',N“' - 三乙酸和膦酸类似物。