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1.One goal in our studies is the synthesis of new
   {5-deaza-and8-deazapteridines}    as folate antagonists.
2.b-dicarbonyl derivatives or a,b-unsaturated aldehydes, were cyclocondensated with different
   {1,3-bisnucleophiles}       , e.g., cyanacetamide(7)or pyrimidine-2,4,6-triamine(14).
3.12was than treated with dimethylformamideand phosphoroxychloride under mild conditions and furtherwithN,N-dimethylammoniumperchlorate to yield the
    {trime-thinium perchlorate}    13, representing a reactive derivative ofmalondialdehyde[19].
4.Recently an alternative preparation of Nor-PTX(3)has been published by condensation14and
      { bromomalondialdehyde}    ,followed by protection of amino groups and Pd-mediated coupling with 2,5-dimethoxybenzyl zinc chloride and final deprotection of the pivaloylated aminogroups[16](Fig. 3)
5. Treatment with dimethylformamide, phos-phoroxychloride and crystallisation with
    {N,N-dimethyl am-monium per chlorate}   gave
    { trimethinium }salt24
6.{Before methotrexate can act as an antitumor agent, an active transport mechanisms into the cell and polyglutamation by the enzyme folypoly-glutamate synthase is necessary.}
7.{Pneumocystis cariniiandToxoplasma gondii}
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1¡¢5-deaza-and 8-deazapteridines£º5 - ÍѵªºÍ8 - Íѵªµûà¤
2¡¢1,3-bisnucleophiles£º1,3- Ë«ºËÊÔ¼Á
3¡¢trime-thinium perchlorate£ºÈýÑǼ׸ßÂÈËáÑÎ
4¡¢bromomalondialdehyde£ºäå±û¶þÈ©
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7¡¢Pneumocystis carinii and Toxoplasma gondii£º¿¨ÊÏ·ÎÄÒ³æºÍ¹­Ðγæ
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ssssllllnnnn

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3Â¥2014-10-08 08:11:53
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yueyue-cc

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4Â¥2014-10-08 11:25:31
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ssssllllnnnn

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4Â¥: Originally posted by yueyue-cc at 2014-10-07 22:25:31
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