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    • 3. 发明授权
    • PNA monomer and precursor
    • PNA单体和前体
    • US07211668B2
    • 2007-05-01
    • US10819769
    • 2004-04-06
    • Sung Kee KimHyunil LeeJong Chan LimSung Hee Lee
    • Sung Kee KimHyunil LeeJong Chan LimSung Hee Lee
    • C07D473/34C07D473/30C07D473/18C07D239/47C07D239/54
    • C07D271/113C07D263/46C07D413/12C07D417/12Y02P20/55
    • This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is sulfur or oxygen; J is nitrogen or C—R′; R1, R′ is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1–C4 alkyl, nitro, nitrile, alkoxy, preferably C1–C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1–C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1–C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.
    • 本申请涉及用于制备PNA(肽核酸)寡聚体的通式(I)的单体,并提供合成预定义的序列PNA寡聚体和随机序列PNA寡聚体的方法:其中E为硫或氧; J为氮或C-R'; R1,R'独立地为H,卤素,烷基,硝基,腈,烷氧基,卤代烷基,卤代烷氧基或具有以下通式之一的官能团:其中A 1, A 3,A 4,A 5 H独立地选自H,卤素如F,Cl,Br或 I,CF 3,烷基,优选C 1 -C 4烷基,硝基,腈,烷氧基,优选C 1〜 卤代(如F,Cl,Br和I)烷基,优选卤代C 1 -C 4烷基,C 1 -C 4烷基, ,卤代(如F,Cl,Br和I)烷氧基,优选卤代C 1 -C 4烷氧基,苯基和卤代(如F,Cl,Br 和I苯基; R2是H或天然或非天然α-氨基酸的保护或未保护的侧链; B是天然或非天然核碱基,其中当所述核碱基具有外来氨基功能时,所述功能受保护基团 不稳定酸,但稳定 在硫醇存在下为弱至中等碱。