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    • 2. 发明申请
    • POLYAZACYCLOALKANE COMPOUNDS
    • 聚环氧烷化合物
    • WO1996028433A1
    • 1996-09-19
    • PCT/GB1996000464
    • 1996-03-01
    • NYCOMED IMAGING A.SCOCKBAIN, JulianSCHULTZE, LisaBULLS, Alan, Ray
    • NYCOMED IMAGING A.SCOCKBAIN, Julian
    • C07D257/02
    • 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是氢或任选被羟基,烷氧基或芳基取代的C 1-12烷基或R是包含N,S,O或P的两亲性芳烷基 间断的C2-25亚烷基链,例如聚环氧烷链或R提供到第二三苄基环系基团的桥,但条件是R不是苄基; X是CHR 1,或其中R是氢,两个X基团可以各自代表CO基团 ; R 1为氢,任选被羟基,烷氧基或羧基取代的C 1-6烷基或烷基部分中具有1至6个碳的芳烷基,并且任选地在芳基部分被烷基,烷氧基,羟基或异硫氰酸酯基取代) 。 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。