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    • 2. 发明授权
    • Preparation of pyrazine derivatives
    • 吡嗪衍生物的制备
    • US4511718A
    • 1985-04-16
    • US471691
    • 1983-03-03
    • Giuseppe RibaldoneMaria G. FelicioliClaudio SantiniGiovanni Agnes
    • Giuseppe RibaldoneMaria G. FelicioliClaudio SantiniGiovanni Agnes
    • C07D241/14C07D241/12C07D241/24C07D401/02C07D413/02C07D417/02
    • C07D241/12C07D241/24
    • A process for the preparation of a pyrazine derivative of the formula ##STR1## wherein R.sub.1 represents hydroxy, C.sub.1 -C.sub.6 alkoxy, or a group of the formula NR.sub.2 R.sub.3 in which R.sub.2 and R.sub.3 are independently a hydrogen atom or C.sub.1 -C.sub.6 alkyl or, together with the nitrogen atom to which they are linked, form a saturated ring having five or six atoms which may contain one or more additional heteroatoms; which process comprises reacting a compound of the formula: ##STR2## wherein R represents a hydrogen atom, C.sub.1 -C.sub.6 alkyl, or C.sub.1 -C.sub.6 alkoxy, Y represents a hydrogen atom or a sodium, lithium, or potassium ion, and A is a nitrile group or a substituent of the formula COR.sub.1 where R.sub.1 is as defined above either with pyruvic aldehyde oxime of the formula: ##STR3## or with a pyruvic aldehyde oxime acetal derivative of the formula: ##STR4## wherein R.sub.4 and R.sub.5 are independently a hydrogen atom or C.sub.1 -C.sub.6 alkyl or may be linked together so that the compound of formula IV is a cyclic acetal; and, when A is a nitrile group, hydrolyzing the reaction product.
    • 制备式I的吡嗪衍生物的方法,其中R 1表示羟基,C 1 -C 6烷氧基或式NR 2 R 3基团,其中R 2和R 3独立地为氢原子或C 1 -C 6烷基, 与它们所连接的氮原子一起形成具有五个或六个原子的饱和环,其可以含有一个或多个另外的杂原子; 该方法包括使下式化合物:其中R表示氢原子,C1-C6烷基或C1-C6烷氧基,Y表示氢原子或钠,锂或钾离子,A为 腈基或式COR1的取代基,其中R 1如上所定义,与下式的丙酮酸肟或与下式的其中R 4和R 5为的丙酮酸肟缩醛衍生物 独立地是氢原子或C 1 -C 6烷基或可以连接在一起,使得式Ⅳ化合物是环状缩醛; 并且当A为腈基时,水解反应产物。