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    • 8. 发明授权
    • Process for preparing substituted 2-cyanopyridines
    • 取代的2-氰基吡啶的制备方法
    • US5258520A
    • 1993-11-02
    • US003648
    • 1993-01-13
    • Wolfgang GienckeJan Vermehren
    • Wolfgang GienckeJan Vermehren
    • C07D213/84C07D215/48C07D217/26C07D221/04C07D213/57
    • C07D213/84C07D215/48C07D217/26C07D221/04
    • Compounds of the formula I ##STR1## in which R.sup.1 is H, alkyl, alkenyl, alkynyl, haloalkyl, alkoxycarbonyl, alkoxyalkyl, phenyl, benzyl or phenoxyalkyl, it being possible for the three latter radicals to be substituted in the phenyl moiety;R.sup.2 is H, alkyl, alkenyl, alkynyl, haloalkyl or alkoxycarbonyl;R.sup.3 is H, alkyl, alkenyl, alkynyl, haloalkyl, alkoxycarbonyl, phenyl, phenoxy, benzyl, it being possible for the three latter radicals to be substituted, or alkoxy; andR.sup.4 is H, alkyl, alkenyl, alkynyl, haloalkyl or alkoxycarbonyl;orR.sup.1 together with R.sup.2 is a saturated chain, and the remaining radicals are as defined above;orR.sup.1 together with R.sup.2 is a chain of the formula --CH.dbd.CH--CH.dbd.CH--, which may be substituted, and the remaining radicals are as defined above;orR.sup.3 together with R.sup.4 is a chain of the formula --CH.dbd.CH--CH.dbd.CH--, which may be substituted, and the remaining radicals are as defined above;are valuable intermediates in the preparation of pharmaceuticals and crop protection agents.The process according to the invention yields compounds of the formula I by reacting a substituted 1-alkoxypyridinium salt of the formula II, ##STR2## in which R.sup.1 to R.sup.4 have the same meaning as in formula I andR.sup.5 is alkyl, alkenyl, alkynyl, benzyl or trialkylsilyl andX is a leaving group;together with a cyanide of the formula IIIM(CN).sub.m (III)in whichM is alkali metal, alkaline earth metal or copper andm is 1 or 2,in a polar, aprotic solvent or mixture of solvents.
    • 其中R 1为H,烷基,烯基,炔基,卤代烷基,烷氧基羰基,烷氧基烷基,苯基,苄基或苯氧基烷基的式I化合物,其后三个基团可以在苯基部分被取代; R2是H,烷基,烯基,炔基,卤代烷基或烷氧基羰基; R3是H,烷基,烯基,炔基,卤代烷基,烷氧基羰基,苯基,苯氧基,苄基,三个后面的基团可以被取代,或烷氧基; R4是H,烷基,烯基,炔基,卤代烷基或烷氧基羰基; 或R 1与R 2一起为饱和链,其余基团如上所定义; 或R 1与R 2一起是式-CH = CH-CH = CH-的链,其可以被取代,其余基团如上所定义; 或R 3与R 4一起是式-CH = CH-CH = CH-的链,其可以被取代,其余基团如上所定义; 是制备药物和作物保护剂的有价值的中间体。 根据本发明的方法通过使式II的取代的1-烷氧基吡啶鎓盐,其中R 1至R 4具有与式I中相同的含义,并且R 5为烷基,链烯基,炔基 苄基或三烷基甲硅烷基,X是离去基团; 连同其中M为碱金属,碱土金属或铜,m为1或2的式III M(CN)m(III)的氰化物在极性,非质子溶剂或溶剂混合物中。
    • 9. 发明授权
    • Aminopyrimidine derivatives, and their use as fungicides
    • 氨基嘧啶衍生物及其作为杀真菌剂的用途
    • US5250530A
    • 1993-10-05
    • US549764
    • 1990-07-09
    • Wolfgang GienckeBurkhard SachseHeinrich Wicke
    • Wolfgang GienckeBurkhard SachseHeinrich Wicke
    • A01N43/54C07D401/04C07D401/14
    • C07D401/04A01N43/54C07D401/14
    • Aminopyrimidine derivatives, their preparation, and agents containing them, and their use as fungicides comprising ##STR1## in which R.sup.1 is alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkynyl, cycloalkylalkyl, substituted aminoalkyl, phenyl, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl or phenoxyphenoxyalkyl, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, or phenyl, R.sup.5 is H, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkoxy, alkylthio, alkoxyalkyl, R.sup.7 R.sup.8 N-,alkylthioalkyl, R.sup.7 R.sup.8 N-alkyl, halogen, alkenyl, alkynyl, phenyl, phenoxy, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl, phenylmercapto, phenylalkoxy or phenylalkylthio, R5 is H, alkyl, alkyloxy, alkenyloxy, alkynyloxy, alkylthio, halogen, or phenyl or R.sup.5 and R.sup.6 together form a chain, and R.sup.7 and R.sup.8 are H, alkyl, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, alkenyl, substituted formyl, phenyl or phenylalkyl, or R.sup.7 or R.sup.8 together with the nitrogen atom form a heterocycle wherein phenyl and cycloalkyl moieties can be substituted, as well as the salts thereof, have advantageous fungicidal properties.
    • 氨基嘧啶衍生物,它们的制备物和含有它们的试剂,以及它们作为杀真菌剂的用途,其包含其中R1是烷基,烷氧基烷基,烷硫基烷基,环烷基,烯基,炔基,环烷基烷基,取代的氨基烷基,苯基,苯基烷基,苯氧基烷基, 苯基巯基烷基或苯氧基苯氧基烷基,R2,R3和R4是H,烷基或苯基,R5是H,烷基,环烷基,环烷基烷基,卤代烷基,烷氧基,烷硫基,烷氧基烷基,R7R8N-,烷硫基烷基,R7R8N-烷基,卤素,烯基,炔基, 苯基,苯氧基,苯基烷基,苯氧基烷基,苯基巯基烷基,苯基巯基,苯基烷氧基或苯基烷硫基,R5是H,烷基,烷氧基,烯氧基,炔氧基,烷硫基,卤素或苯基,或R5和R6一起形成链,R7和R8是H, 烷基,烷氧基烷基,羟基烷基,烷硫基烷基,烯基,取代的甲酰基,苯基或苯基烷基,或R7或R8与氮原子一起形成杂环,其中苯基和环烷基部分也可被取代 作为其盐具有有利的杀真菌性质。