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    • 24. 发明授权
    • Fungicidal 1-aminomethyl-3-(2-fluoro-3-chlorophenyl)-4-cyanopyrrole
derivatives
    • 杀真菌剂1-氨基甲基-3-(2-氟-3-氯苯基)-4-氰基吡咯衍生物
    • US4973350A
    • 1990-11-27
    • US307390
    • 1989-02-06
    • Detlef WollweberWilhelm Brandes
    • Detlef WollweberWilhelm Brandes
    • A01N43/36A01N43/40C07D207/34C07D401/12C07D403/06C07D405/12C07D409/12
    • C07D401/12A01N43/36A01N43/40C07D207/34C07D405/12
    • Fungicidal 1-aminomethyl-3-(2-fluoro-3-chlorophenyl)-4-cyano-pyrrole derivatives of the formula ##STR1## in which R stands for a ##STR2## wherein R.sup.1 stands for optionally substituted alkyl, for alkenyl, alkinyl or cycloalkyl, or for in each case optionally substituted aralkyl or aryl,R.sup.2 stands for in each case optionally substituted heterocyclylalkyl, heterocyclylalkenyl, heterocyclylalkinyl or heterocyclyl, for dialkylaminoalkyl or for in each case optionally substituted cycloalkylalkyl or phenethyl,R.sup.3 stands for hydrogen or alkyl andR.sup.4 stands for cyano, alkanoyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, for alkylsulphinyl, for alkylsulphonyl, for phenylsulphinyl or for phenylsulphonyl.The compound where R is replaced by an election-withdrawing leaving group is a novel intermediate.
    • 式(I)的杀真菌剂1-氨基甲基-3-(2-氟-3-氯苯基)-4-氰基 - 吡咯衍生物,其中R代表一个,其中R1代表任选取代的 烷基,对于链烯基,炔基或环烷基,或者在每种情况下均为任选取代的芳烷基或芳基,R 2在每种情况下表示任选取代的杂环基烷基,杂环基烯基,杂环基炔基或杂环基,对于二烷基氨基烷基或在每种情况下任选取代的环烷基烷基或苯乙基,R 3 代表氢或烷基,R4代表氰基,烷酰基,烷氧基羰基,烷基氨基羰基,二烷基氨基羰基,烷基亚磺酰基,烷基磺酰基,苯基亚磺酰基或苯基磺酰基。 其中R由选举撤离离去基团代替的化合物是新的中间体。
    • 28. 发明授权
    • Process for the preparation of 3-cyano-4-aryl-pyrroles
    • 3-氰基-4-芳基吡咯的制备方法
    • US4912229A
    • 1990-03-27
    • US197065
    • 1988-05-19
    • Detlef Wollweber
    • Detlef Wollweber
    • C07B61/00C07D207/22C07D207/34
    • C07D207/22C07D207/34
    • A process for the preparation of a 3-cyano-4-aryl-pyrrole of the formula ##STR1## in which Ar is optionally substituted heteroaryl or aryl, which comprises (a) reacting an .alpha.-cyanoacrylic acid derivative of the formula ##STR2## in which R.sup.1 is amino or alkoxy, with an isocyanoacetic acid ester of the formula ##STR3## in which R.sup.2 is alkyl, in the presence of a base thereby to produce a .DELTA..sup.2 -pyrroline-2-carboxylic acid derivative of the formula ##STR4## in which X represents hydrogen or an equivalent of an inorganic or organic cation,and (b) oxidatively decarboxylating the .DELTA..sup.2 -pyrroline-2-carboxylic acid. The end products are known fungicides and the intermediates IVa are new and themselves fungicidally active.
    • 制备式(I)的3-氰基-4-芳基吡咯的方法,其中Ar是任选取代的杂芳基或芳基,其包括(a)使式(I)的α-氰基丙烯酸衍生物与式 其中R 1是氨基或烷氧基,与式(III)的异氰酸乙酸酯(其中R 2是烷基)在碱的存在下反应,生成DELTA 2-吡咯啉-2 (IVa)的羧酸衍生物,其中X表示氢或当量的无机或有机阳离子,和(b)使DELTA 2-吡咯啉-2-羧酸氧化脱羧。 最终产品是已知的杀真菌剂,中间体IVa是新的并且其本身具有杀真菌活性。