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    • 6. 发明申请
    • Methods and Intermediates for the Synthesis of 4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazines
    • 用于合成4-氧代-3,4-二氢 - 咪唑并[5,1-d] [1,2,3,5]四嗪的方法和中间体
    • US20130012706A1
    • 2013-01-10
    • US13581874
    • 2011-02-25
    • Marc Geoffery HummersoneDavid Cousin
    • Marc Geoffery HummersoneDavid Cousin
    • C07D487/04
    • C07D487/04
    • The present invention provides a compound of general formula (II), or a salt or solvate thereof: wherein A is independently -A1, -A2, -A3, -A4, -A5, -A6, or -A7, wherein: -A1 is independently C5-12heteroaryl, and is optionally substituted; -A2 is independently thioamido or substituted thioamido; -A3 is independently imidamido, substituted imidamido, N-hydroxyimidamido, or substituted N-hydroxyimidamido; -A4 is independently hydroxamic acid or hydroxamate; -A5 is independently carboxamide or substituted carboxamide; -A6 is independently aliphatic C2-6alkenyl, and is optionally substituted; and -A7 is independently carboxy or C1-4alkyl-carboxylate; and its use in the synthesis of temozolomide and analogues thereof.
    • 本发明提供通式(II)的化合物或其盐或溶剂合物:其中A独立地为-A1,-A2,-A3,-A4,-A5,-A6或-A7,其中:-A1 独立地是C 5-12杂芳基,并且任选被取代; -A2独立地是硫代酰氨基或取代的硫代酰氨基; -A3独立地是亚氨酰胺基,取代的亚氨代酰氨基,N-羟基亚氨基酰胺基或取代的N-羟基亚氨基酰胺基; -A4独立为异羟肟酸或异羟肟酸盐; -A5独立地是甲酰胺或取代的甲酰胺; -A6独立地是脂族C 2-6烯基,并且是任选取代的; -A7独立地是羧基或C1-4烷基 - 羧酸酯; 及其在替莫唑胺及其类似物合成中的应用。