CAS: 461-88-1; Pyridine-2,4-Diamine

该化合物是有机化合物,其特征是2和4个位置用两组氨基氨基环替换成2个环,似乎是白色到浅黄色晶状固体,在水和有机溶剂中溶解,反映其因氨基组的存在而具有极性,该化合物主要以其作为制药剂的作用而闻名,特别是在治疗Lambert-Eaton甲状腺综合症等某些...

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1266119-48-5 4487-50-7 14916-64-4

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pyridine pyridine2,4-bis(ethoxycarbonyl)aminopyridine 2,4-Diamino-5-pyridincarbonsaeure 2-bromo-3-cyano-4,6-diamino-pyridine2,4-diamino-3-fluoropyridine 2,4-diamino-3-bromopyridine 2,4-diamino-3,5-dibromopyridine 17H15N5O2C17H15N5O2

合成工艺路线路线简述

    2,4-Bis<(Ethoxycarbonyl)Amino>Pyridine置于氢氧化钾体系中,用 乙醇 作为反应溶剂,化学反应 6.0H,以70%的收率获得产物2,4-二氨基吡啶
    参考文献:2,4-二氨基-5-苄基嘧啶和类似物作为抗菌剂.3.氨基吡啶与酚曼尼希碱的c-苄基化.合成甲氧苄啶的1和3脱氮类似物.
    标题:2,4-二氨基-5-苄基嘧啶和类似物作为抗菌剂.3.氨基吡啶与酚曼尼希碱的c-苄基化.合成甲氧苄啶的1和3脱氮类似物.
    摘要:2,4-二氨基-4-[(n,N-二甲基氨基)甲基]苯酚和卤素(溴和氟)的2,4-二氨基吡啶亲电取代产生3-苄基和3-卤代衍生物,以及少量衍生物在3,5职位上的混乱状况.用酚曼尼希碱处理2,4-二氨基-3-卤代吡啶得到5-和n-苄基化.2,4-二氨基-3-溴-5-(4-羟基-3,5-二甲氧基苄基)吡啶在酚基上甲基化,产率高,然后脱卤反应生成3-脱氮杂甲氧苄啶[2,4-二氨基-5-(3,4,5-三甲氧基苄基)吡啶].该化合物作为大肠杆菌二氢叶酸还原酶抑制剂的活性比甲氧苄氨嘧啶低约300倍.2,6-二氨基吡啶很容易被酚曼尼希碱在3,5位以及氨基上二苄基化;使用四倍过量的吡啶以50%的产率提供了3-苄基化的2,6-二氨基吡啶.在10(-4)m时,它不能作为二氢叶酸还原酶的抑制剂.在此处报道的条件下,2-氨基吡啶和4-氨基吡啶不会产生c-苄基化产物.
    DOI:10.1021/jm00178A008

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    专利信息


    专利号:US-2006009642-A1
    优先权日:2001-10-12
    标题 :Methods for the synthesis of substituted purines
    发明人:DING SHENG; DING QIANG; GRAY NATHANAEL S; SCHULTZ PETER G
    权利人:IRM LLC
    摘要:The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines.

    专利号:US-6949644-B2
    优先权日:2001-10-12
    标题 :Methods for the synthesis of substituted purines
    发明人:DING SHENG; DING QIANG; GRAY NATHANAEL S; SCHULTZ PETER G
    权利人:SCRIPPS RESEARCH INST
    摘要:The invention provides general methods for preparing 2,9-, 2,6,9-, O 6 -aryl- and O 6 -alkyl-substituted purines in a combinatorial and traceless fashion. The methods involve, in some embodiments, Mitsunobu alkylation of 2-fluoro-6-phenylsulfenylpurine at N9 with alcohols in solution, followed by C2-capture of the purine core with a resin-bound amine and subsequent oxidation and displacement of the C6 sulfonyl group with amines and anilines. In one aspect, the present invention provides a method of preparing a 2,6,9-substituded purine compounds of Formula I: n n nthe method comprising:n a) oxidizing a resin-bound compound of Formula II: n n to provide a resin-bound compound of Formula III: n n b) reacting the compound of Formula III with an amine of Formula IVn nNR 3 R 4   IV,n nto provide a resin-bound compound of Formula V n n c) cleaving the resin-bound compound of Formula V from the resin to provide the substituted purine compounds of Formula I.

    专利号:US-4031106-A
    优先权日:1973-12-19
    标题:Synthesis of aromatic amines by reaction of aromatic compounds with ammonia
    发明人:DELPESCO THOMAS WAYNE
    权利人:DU PONT
    摘要:An improved process is provided for producing an aromatic amine from ammonia and an aromatic compound which comprises reacting the aromatic compound with ammonia at a temperature of from about 150 DEG C. to about 500 DEG C. and at a pressure of from about 10 to about 1000 atmospheres in the presence of a conditioned nickel/nickel oxide/zirconium oxide cataloreactant containing an oxide of lanthanum, samarium, holmium, europium, erbium, yttrium, praseodymium, neodymium, terbium, ytterbium, dysprosium or a mixture of any of them.

    专利号:US-3929889-A
    优先权日:1971-02-16
    标 题 :Synthesis of aromatic amines by reaction of aromatic compounds with ammonia
    发明人:SQUIRE EDWARD NOONAN
    权利人:DU PONT
    摘要:An improved process for producing an aromatic amine is provided in which an aromatic compound is reacted with ammonia in the presence of a conditioned nickel/nickel oxide cataloreactant at a temperature of from about 150*C. to about 500*C. and at a pressure of from about 10 to about 1000 atmospheres.

    专利号:US-4001260-A
    优先权日:1973-12-19
    标 题:Synthesis of aromatic amines by reaction of aromatic compounds with ammonia
    发明人:DEL PESCO THOMAS W
    权利人:DU PONT
    摘要:An improved process is provided for producing an aromatic amine from ammonia and an aromatic compound which comprises reacting the aromatic compound with ammonia at a temperature of from about 150° C. to about 500° C. and at a pressure of from about 10 to about 1000 atmospheres in the presence of a conditioned nickel/nickel oxide/zirconium oxide cataloreactant which has been treated with ammonia prior to introduction of the cataloreactant to the amination reactants.

    专利号:US-2003171583-A1
    优先权日:2001-10-12
    标 题 :Methods for the synthesis of substituted purines
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    摘要:Journal of Medicinal Chemistry., 8(296), 1965
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