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    • 74. 发明申请
    • PROCESS FOR PREPARATION OF PYRIMIDINONE DERIVATIVES
    • 制备吡咯烷酮衍生物的方法
    • WO99067202A1
    • 1999-12-29
    • PCT/EP1999/004188
    • 1999-06-17
    • C07C271/68C07D213/82C07D239/96C07D333/38C07D333/68C07D495/04
    • C07D213/82C07C271/68C07D239/96C07D333/68C07D495/04
    • A process for the preparation of compounds having plant protecting, in particular fungicidal properties, of the formula (I), wherein A is a fused 5-membered heterocyclic ring which may be saturated or unsaturated, aromatic or non-aromatic and which may contain one or two hetero atoms O, S and/or N, or is fused benzo, pyrido or pyridazino; R1 and R2 are groups which are inert to the reactions; R3 is optionally substituted C1-C8alkyl, C2-C8alkenyl, C2-C8alkynyl, C3-C6cycloalkyl or C3-C6cycloalkyl-C1-C6alkyl; and R4 is optionally substituted C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl or C3-C6cycloalkyl-C1-C6alkyl; in which process (a) a compound of the formula (II), wherein A, R1, R2 and R3 are as defined for formula (I), is reacted with an orthocarbonate of the formula (III), wherein R4 is as defined for the formula (I) and Y is OR4, CN or NO2, to give the intermediate compound of formula (IV); and subsequently (b) the compound of the formula (IV) is cyclized to a compound of the formula (I).
    • 一种制备具有式(I)的植物保护,特别是杀真菌性的化合物的方法,其中A是可以是饱和或不饱和的,芳族或非芳族的并且可以含有一个的稠合的5元杂环 或两个杂原子O,S和/或N,或稠合苯并,吡啶或哒嗪; R1和R2是对反应呈惰性的基团; R 3是任选取代的C 1 -C 8烷基,C 2 -C 8烯基,C 2 -C 8炔基,C 3 -C 6环烷基或C 3 -C 6环烷基-C 1 -C 6烷基; 且R 4是任选取代的C 1 -C 6烷基,C 2 -C 6烯基,C 2 -C 6炔基,C 3 -C 6环烷基或C 3 -C 6环烷基-C 1 -C 6烷基; 其中方法(a)其中A,R 1,R 2和R 3如式(I)所定义的式(II)化合物与式(III)的原碳酸酯反应,其中R 4如 式(I)和Y是OR 4,CN或NO 2,得到式(IV)的中间体化合物; 然后(b)将式(Ⅳ)化合物环化成式(I)化合物。
    • 77. 发明专利
    • BR9911367A
    • 2001-03-13
    • BR9911367
    • 1999-06-17
    • NOVARTIS AG
    • WALTER HARALD
    • C07C271/68C07D213/82C07D239/96C07D333/38C07D333/68C07D495/04
    • A process for the preparation of compounds having plant protecting, in particular fungicidal properties, of the formula I wherein A is a fused 5-membered heterocyclic ring which may be saturated or unsaturated, aromatic or non-aromatic and which may contain one or two hetero atoms O, S and/or N, or is fused benzo, pyrido or pyridazino; R1 and R2 are groups which are inert to the reactions; R3 is optionally substituted C1-C8alkyl, C2-C8alkenyl, C2-C8alkynyl, C3-C6cycloalkyl or C3-C6 cycloalkyl-C1-C6alkyl; and R4 is optionally substituted C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl or C3-C6 cycloalkyl-C1-C6alkyl; in which process (a) a compound of the formula II, wherein A, R1, R2 and R3 are as defined for formula I, is reacted with an orthocarbonate of the formula III, wherein R4 is as defined for formula I and Y is OR4, CN or NO2, to give the intermediate compound of formula IV; and subsequently (b) the compound of the formula IV is cyclized to a compound of the formula I