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    • 5. 发明授权
    • Process for preparing triazolopyrimidine derivatives
    • 制备三唑并嘧啶衍生物的方法
    • US06570014B1
    • 2003-05-27
    • US10134504
    • 2002-04-30
    • Chien-Hsing ChenChun-Lin YehYu-Hwa Chuang
    • Chien-Hsing ChenChun-Lin YehYu-Hwa Chuang
    • C07D48704
    • C07D487/04
    • A process for preparing triazolopyrimidine derivatives of the formula (I): wherein R1 represents a hydrogen or an alkyl radical of one to ten carbon atoms, or a cycloalkyl radical of three to six carbon atoms, or an alkenyl radical of up to four carbon atoms; R2 represents a hydrogen, a halogen atom, a hydroxyalkyl or alkyl radical of one to ten carbon atoms; R3 represents a hydrogen, a hydroxyalkyl or alkyl radical of one to four carbon atoms; by rapidly preparing diamino-1,2,4-triazole which is reacted with an aldehyde to form an imide which is reacted with an &agr;,&bgr;-unsaturated acid derivative, the reaction product of which is hydrolyzed in the presence of an acid to produce the triazolopyrimidine derivatives of formula (I). The compounds of the formula (I) are capable of preventing bronchospasm.
    • 制备式(I)的三唑并嘧啶衍生物的方法:其中R 1表示氢或1至10个碳原子的烷基或具有3至6个碳原子的环烷基或至多4个碳原子的烯基 ; R2表示氢原子,卤素原子,1-10个碳原子的羟烷基或烷基; R3表示氢原子,1-4个碳原子的羟烷基或烷基; 通过快速制备与醛反应以形成与α,β-不饱和酸衍生物反应的酰亚胺的二氨基-1,2,4-三唑,其反应产物在酸的存在下水解以产生 式(I)的三唑并嘧啶衍生物。 式(I)的化合物能够防止支气管痉挛。