CAS: 169287-79-0; 2-(2-(((Benzhydryloxy)Carbonyl)Amino)-6-Oxo-1H-Purin-9(6H)-yl)Acetic Acid

该化合物是属于纯衍生物类的合成有机化合物,该化合物具有纯核心特征,其特点是含有氮原子的引信双环结构,有助于其生物活动;二苯氧碳基组的存在会加强其脂性,并可能影响其与生物目标的相互作用;其结构中的箱状酸功能组表示形成盐类或酯类的潜力,这可能影响其溶性与稳定性;该化合物可能具有药用化学特性,特别是治疗剂的开发.其具体特性,如熔点,溶性,再活性,将取决于分子相互作用和研究的环境.

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169287-69-8 186046-80-0 1028077-12-4

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CAS号91-01-0 二苯甲醇 | CAS号10310-21-1 2-氨基-6-氯嘌呤 | CAS号169287-67-6 2-Amino-6-chlor...

合成工艺路线路线简述

    📜Benzyl 2-Amino-6-Chloropurine-9-Acetate置于sodium Hydride,N,N-二异丙基乙胺,3-羟基丙腈体系中,用 四氢呋喃 用作溶剂,化学反应 12.5H,反应生成(2-二苯甲基氧基羰基氨基-6-氧代-1,6-二氢嘌呤-9-基)-乙酸
    参考文献:叠氮肽核酸.固相肽核酸(pna)合成的替代策略.
    标题:叠氮肽核酸.固相肽核酸(pna)合成的替代策略.
    摘要:[反应:见正文]报道了一种使用叠氮基团掩盖n端的pna合成的实用有效方法.脱保护在5分钟内进行,而偶联在60分钟内完成.膦脱保护的接近中性条件,再加上使用羟基苯并三唑活化的单体的无碱偶联,使得该方法非常温和.
    Doi:10.1021/ol0358408

    海关参考信息

    专利信息


    专利号:US-6172226-B1
    优先权日:1993-12-22
    标 题:Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions
    发明人:COULL JAMES M; EGHOLM MICHAEL; HODGE RICHARD P; ISMAIL MOHAMED; RAJUR S B
    权利人:PERSEPTIVE BIOSYSTEMS INC
    摘要:A method is disclosed for preparing novel PNA synthons having protecting groups capable of removal under mild conditions. The PNA synthons are prepared by coupling novel N-substituted nucleobase intermediates having carbamate protection of the exocyclic amino group of the heterocycle to an amino protected backbone or an amino protected backbone ester of the amino acid N-(2-aminoethyl)-glycine. By the method of this invention, the resultant PNA synthons can have orthogonal protection of the carbamate protected nucleobase and the amino protected backbone. The PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. Novel compositions of matter are also disclosed. In addition, a guanine PNA synthon having selective carbamate protection of the exocyclic 2-amino group with the C6 carbonyl group unprotected is disclosed.

    专利号:US-7211668-B2
    优先权日:2003-07-28
    标 题 :PNA monomer and precursor
    发明人:KIM SUNG KEE; LEE HYUNIL; LIM JONG CHAN; LEE SUNG HEE
    权利人:PANAGENE INC
    摘要: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: n nwhereinn 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: n nwhereinn A 1 , A 2 , A 3 , A 4 , A 5 , is independently selected from H, halogen such as F, Cl, Br or I, CF 3 , alkyl, preferably C 1 –C 4 alkyl, nitro, nitrile, alkoxy, preferably C 1 –C 4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C 1 –C 4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C 1 –C 4 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.

    专利号:US-7411065-B2
    优先权日:2002-04-26
    标 题 :PNA monomer and precursor
    发明人:KIM SUNG KEE; LEE HYUNIL; LIM JONG CHAN; CHOI HOON; JEON JAE HOON; AHN SANG YOUL; LEE SUNG HEE; YOON WON JUN
    权利人:PANAGENE INC
    摘要:This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oglimers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: n nwhereinn E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 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.

    专利号:US-7022851-B2
    优先权日:2002-01-24
    标题 :PNA monomer and precursor
    发明人:KIM SUNG KEE; LEE HYUNIL; LIM JONG CHAN; CHOI HOON; JEON JAE HOON; AHN SANG YOUL; LEE SUNG HEE
    权利人:PANAGENE INC
    摘要: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: n nwhereinn R1, R2, R3, R4, R5 is independently H, halogen, C 1 –C 4 alkyl, nitro, nitrile, C 1 –C 4 alkoxy, halogenated C 1 –C 4 alkyl, or halogenated C 1 –C 4 alkoxy, wherein at least one of R1, R3, and R5 is nitro; R6 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.

    专利号:EP-1873156-A1
    优先权日:1995-06-07
    标 题:Process for the preparation of 6-[[(alkoxy)carbonyl]amino]-9H-Purine-9-acetic acid and 4-[(alkoxycarbonyl)amino]-2-oxo-1(2H)-Pyrimidineacetic acid derivatives as synthons for the synthesis of peptide nucleic acids

    专利号:US-6133444-A
    优先权日:1993-12-22
    标 题 :Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions

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    主要参考文献

    参考标题: Pna Monomer And Precursor Monomere Et Precurseur Pna
    摘要:This Application Relates To Monomers Of The General Formula (I) For The Preparation Pna (Peptide Nucleic Acid) Oligomers And Provides Method For The Synthesis Of Both Predefined Sequence Pna Oligomers And Random Sequence Pna Oligomers: (I) Wherein E Is Nitrogen Or C-R'; J Is Sulfur Or Oxygen; R', Rl, R2, R3, R4 Is Independently H, Halogen, Alkyl, Nitro, Nitrile, Alkoxy, Halogenated Alkyl, Halogenated Alkoxy, Phenyl Or Halogenated Phenyl, Rs Is H Or Protected Or Unprotected Side Chain Of Natural Or Unnatural A-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.

    合成参考文献

    参考DOI号:10.1021/ol0358408
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