药物/荧光染料缀合体前体-β(3-羧基伞形酮)-D-半乳糖苷钾盐的合成  

Synthesis of the Precursor of Drug/Fluorescent Dye Conjugate-Potassium Salt of β-[7(3-Carboxycoumarinoxy)] D-Galactoside

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作  者:孙廷辉 骆文莹[1] 包晓春 刘志强[1] 

机构地区:[1]浙江医科大学药学系,杭州310006

出  处:《现代应用药学》1990年第6期21-23,共3页

摘  要:本文介绍药物/荧光染料缀合体前体-β(3-羧基伞形酮)-D-半乳糖营钾盐的合成方法。以D-半乳糖为原料,经酯化,溴代制得a-溴-四乙酰半乳糖(I),另以2,4-二羟基苯甲醛为原料,与丙二酸二乙酯在哌啶的催化作用下经过Knoevenagel缩合反应,再环合成3-乙氧甲酰基7-羟基香豆(I)。然后将(I)和(I)连接再脱去乙酰基即制得药物/荧光染料缀合体前体-β(3-羧基伞形酮)-D-半乳糖苷(Ⅱ)钾盐。In this paper, we described the synthesis of a precursor of the drug/fluorescent dye conjugate-potassium salt of β-〔7(3-Carboxycoumarinoxy)〕D-galactoside. Raw material, D-galactose wasacetylated and brominated to form a-bromo-tetraacetyl galactose (I); another starting material,2.4 dihydroxybenzaldehyde underwent a Knoevenagel condensation with diethylmalonate in aceticacid and a catalyst-piperidine forming 3-carboethoxy-7-hydroxycoumarin (Ⅱ). The final product,Potassium salt of β-〔7(3-Carboxycoumarinoxy)〕-D-galactoside was prepared by a conjugation of(Ⅰ) and (Ⅱ) and followed by the deacetylation of its intermediate.

关 键 词:底物标记抗原 荧光免疫检测 

分 类 号:R981.9[医药卫生—药品]

 

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