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    • 10. 发明授权
    • Coumarin-labeled nucleoside 5'-triphosphates
    • 香豆素标记核苷5'-三磷酸
    • US5587472A
    • 1996-12-24
    • US460027
    • 1995-06-02
    • Nanibhushan DattaguptaJurgen Kocher
    • Nanibhushan DattaguptaJurgen Kocher
    • C07H21/00C07H19/10C07H19/20C07H21/04
    • C07H21/00
    • A fluorescent label compound having the formulaA--B.sup.1 --B.sup.2 --B.sup.3 --CwhereinA represents the residue of a natural or synthetic nucleotide or nucleoside or a derivative thereof;B.sup.1 represents a divalent spacer radical or a single bond;B.sup.2 represents a divalent spacer radical;B.sup.3 represents a divalent spacer radical or a single bond; andC represents a coumarin radical having the formula ##STR1## in which R.sup.1 represents hydrogen or cyano;R.sup.2 represents phenyl or thiazolyl bonded in the 2-, 4- or 5-position, wherein the phenyl is unsubstituted or substituted by nitro, cyano, amino, --NH--C.sub.1-4 -alkyl, --(CH.sub.2).sub.1-4 --NH.sub.2, --(CH.sub.2).sub.1-4 --NH--(CH.sub.2).sub.1-3 --CH.sub.3, carboxy, C.sub.1-4 -alkoxycarbonyl, C.sub.1-4 -alkoxycarbonyloxy, hydroxy, C.sub.1-4 -alkylaminocarbonyl, or C.sub.1-4 -alkylcarbonylamino and either further unsubstituted or substituted by C.sub.1-4 -alkyl, fluorine, chlorine or bromine, and where the thiazolyl is unsubstituted or monosubstituted or disubstituted by chlorine, cyano, carboxyl, or C.sub.1-4 -alkoxycarbonyl, or the thiazolyl is fused in the 4- and 5-position with a benzene ring which is either unsubstituted or substituted by carboxyl, amino, or hydroxyl;R.sup.3 represents hydrogen, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxycarbonyl-C.sub.1-4 -alkyl, or phenylsulphonyl, where the C.sub.1-4 -alkyl is unsubstituted or substituted by hydroxyl, amino, carboxyl, or C.sub.1-4 -alkoxycarbonyl, and where the phenylsulphonyl is unsubstituted or monosubstituted or disubstituted by chlorine, bromine, or C.sub.1-4 -alkyl;or where one of the radicals R.sup.2 or R.sup.3 denotes or is substituted by a primary or secondary amino group, hydroxyl, carboxyl, or C.sub.1-4 -alkoxycarbonyl, or can be converted into such a group by hydrolysis or hydrogenation.
    • 具有式A-B1-B2-B3-C的荧光标记化合物,其中A表示天然或合成的核苷酸或核苷或其衍生物的残基; B1代表二价间隔基团或单键; B2表示二价间隔基; B3表示二价间隔基或单键; 并且C表示具有式“IMAGE”的香豆素基团,其中R 1表示氢或氰基; 氰基,氨基,-NH-C 1-4 - 烷基, - (CH 2)1-4-NH 2,其中苯基未被取代或被硝基,氰基,氨基, , - (CH 2)1-4-NH-(CH 2)1-3 -CH 3,羧基,C 1-4 - 烷氧基羰基,C 1-4 - 烷氧基羰基氧基,羟基,C 1-4 - 烷基氨基羰基或C 1-4 - 烷基羰基氨基 进一步未取代或被C 1-4 - 烷基,氟,氯或溴取代,并且其中噻唑基未被取代或被氯,氰基,羧基或C 1-4 - 烷氧基羰基单取代或二取代,或噻唑基稠合在4- 和5-位,其中苯环是未取代的或被羧基,氨基或羟基取代; R 3表示氢,C 1-4 - 烷基,C 1-4 - 烷氧基羰基-C 1-4 - 烷基或苯基磺酰基,其中C 1-4 - 烷基未被取代或被羟基,氨基,羧基或C 1-4 - 烷氧基羰基取代, 并且其中苯基磺酰基未被取代或被氯,溴或C 1-4 - 烷基单取代或二取代; 或其中一个基团R 2或R 3表示或被伯或仲氨基,羟基,羧基或C 1-4 - 烷氧基羰基取代,或者可以通过水解或氢化转化为该基团。