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    • 22. 发明授权
    • Coumaranedione-3-monoximes
    • 香豆酮-3单肟
    • US3993666A
    • 1976-11-23
    • US495550
    • 1974-08-08
    • Hermann OedigerRudolf Braden
    • Hermann OedigerRudolf Braden
    • C07D307/83C07D493/00
    • C07D307/83
    • Coumaranedione-3-monoximes which may be substituted in the benzene ring by halo or alkyl. The compounds are obtained by treating the corresponding 2-hydroxyphenylacetic acid lactone with nitrous acid or with an ester, salt or chloride of nitrous acid in an acid medium. The coumaranedione-3-monoxime thus obtained is an intermediate which undergoes hydrogenation in the presence of a suitable acid anhydride to afford the corresponding 3-amidocoumaranone, which compound, upon hydrolysis in the presence of dilute acid, affords the corresponding .alpha.-amino-2-hydroxyphenylacetic acid. That product is also an intermediate which has utility in the synthesis of antibiotics, including cephalosporin and penicillin derivatives.
    • 可以在苯环中被卤素或烷基取代的甘油二酮-3-单肟。 该化合物通过在酸性介质中用亚硝酸或亚硝酸的酯,盐或氯化物处理相应的2-羟基苯基乙酸内酯而获得。 由此获得的香豆素二酮-3-肟是在合适的酸酐存在下进行氢化得到相应的3-氨基香豆素的中间体,该化合物在稀酸存在下水解时,得到相应的α-氨基-2 - 羟基苯乙酸。 该产品也是在抗生素合成中具有用途的中间体,包括头孢菌素和青霉素衍生物。