6-(1,3-benzodioxy-5-(methyl)-substituted uracil derivative, synthesis method and application thereof, and medicine

The invention discloses a 6-(1,3-benzodioxo-5-(methyl))-substituted uracil derivative, a synthesis method and application thereof, and a drug, wherein the structural general formula is represented bya formula I, n is equal to 0 or 1, R1 is selected from C1-C3 alkyl, and R2 is any one selected from a...

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Hauptverfasser: HE YANPING, ZHANG RUIHAN, LUO RONGHUA, ZHENG YONGTANG, ZHANG XINGJIE, LI XIAOLI, LI YIMING, QIN HUAYAN, XIAO WEILIE, YANG LIUMENG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a 6-(1,3-benzodioxo-5-(methyl))-substituted uracil derivative, a synthesis method and application thereof, and a drug, wherein the structural general formula is represented bya formula I, n is equal to 0 or 1, R1 is selected from C1-C3 alkyl, and R2 is any one selected from allyl, a group with a structural formula represented by a formula (1) and a group with a structuralformula represented by a formula (2). According to the invention, by using an S-DABO compound and a diphenylamine ester compound SPJ-L-5 as lead materials, based on a pharmacophore splicing and molecular heterozygosis drug molecule design strategy, a core pharmacophore 1,3-benzodioxy of SPJ-L-5 is introduced into a C-6 site of a pyrimidine ring of an S-DABO compound while a preferred group at a C-2 site is reserved, so that excellent anti-HIV drug candidates with broad spectrum, high efficiency and moderate price are developed. 本申请公开了一种6-(1,3-苯并二氧基-5-(甲)基)-取代尿嘧啶衍生物、合成方法、应用、药物,具有结构通式如式I:其中,n=0或1;R选自C~C的烷基;R选自烯丙基、具有式(1)所