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    • 20. 发明授权
    • Process for the preparation of 10-deazaaminopterin and related compounds
    • 制备10-脱甲氨蝶呤及相关化合物的方法
    • US4172200A
    • 1979-10-23
    • US915584
    • 1978-06-15
    • James R. PiperJohn A. Montgomery
    • James R. PiperJohn A. Montgomery
    • C07D475/08
    • C07D475/08
    • There is disclosed an improved process for the preparation of 10-deazaaminopterin and related compounds. In accordance with this process, 6-(bromomethyl)-2,4-pteridinediamine hydrobromide is reacted with triphenylphosphine to form a phosphonium salt which is then treated with a base to yield the corresponding ylid (2,4-diamino-6-pteridinyl)methylenetriphenylphosphorane. This compound is reacted with an aromatic aldehyde such as diethyl 4-formylbenzoyl-L-glutamate to form an olefin which is then reduced catalytically to the tetrahydro derivative of the desired product. Oxidation of the tetrahydro derivative is accomplished with hydrogen peroxide.
    • {PG,1公开了一种用于制备10-脱氮氨基蝶呤及相关化合物的改进方法。 根据该方法,使6-(溴甲基)-2,4-喋啶二胺氢溴酸盐与三苯基膦反应形成鏻盐,然后用碱处理,得到相应的内联(2,4-二氨基-6-吖啶基) 亚甲基三苯基正膦。 该化合物与芳醛如4-甲酰基苯甲酰基-L-谷氨酸二乙酯反应,形成烯烃,然后将该烯烃催化还原成所需产物的四氢衍生物。 四氢衍生物的氧化是用过氧化氢完成的。