PROCESS FOR THE SYNTHESIS OF MANDIPROPAMID AND DERIVATIVES THEREOF
    1.
    发明申请
    PROCESS FOR THE SYNTHESIS OF MANDIPROPAMID AND DERIVATIVES THEREOF 审中-公开
    合成麦芽苦苷及其衍生物的方法

    公开(公告)号:WO2007020381A3

    公开(公告)日:2007-05-03

    申请号:PCT/GB2006002946

    申请日:2006-08-08

    Abstract: A process for the preparation of a compound of formula (I) wherein: R is an alkynyl group; R 1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, phenyl and phenylalkyl, it being possible in turn for all of the receding groups to carry one or more identical or different halogen atoms; alkoxy; alkenyloxy; alkynyloxy; alkoxyalkyl; haloalkoxy; alkylthio; haloalkylthio; alkysulfonyl; formyl; alkanoyl; hydroxy; halogen; cyano; nitro; amino; alkylamino; dialkylamino; carboxyl; alkoxycarbonyl; alkenyloxycarbonyl; or alkynyloxycarbonyl; and n is an integer from 0 to 3, said process comprising: (i) the reaction of a compound of formula (III) wherein R, R 1 and n are as hereinbefore defined; m and m' are independently 0 or 1; when m and m' are both 0, A is an alkyl, alkenyl or alkynyl group (suitably having up to eight carbon atoms), optionally substituted by one or more groups independently selected from halogen, hydroxy, alkoxy, C 1-4 dialkylamino or cyano; when one of m and m' is 0 and the other is 1, A is an alkanediyl, alkenediyl or alkynediyl group containing at least two carbon atoms (and suitably having up to eight carbon atoms), optionally substituted by one or more groups independently selected from halogen, hydroxy, alkoxy, C 1-4 dialkylamino or cyano; when m and m' are both 1, A is an alkanetriyl, alkenetriyl or alkynetriyl group containing at least three carbon atoms (and suitably having up to eight carbon atoms), optionally substituted by one or more groups independently selected from halogen, hydroxy, alkoxy, C 1-4 dialkylamino or cyano; and wherein if the group A contains three or more carbon atoms, one or more of the carbon atoms may each optionally be replaced with an oxygen atom, provided that there is at least one carbon atom between any two oxygen atoms in the molecule, with a compound of formula (IV) to give a compound of formula (II) wherein R, R 1 and n are as hereinbefore defined, and (ii) the reaction of a compound of formula (II) with , wherein L is a leaving group, to give the compound of formula (I) as hereinbefore defined, is disclosed.

    Abstract translation: 一种制备式(I)化合物的方法,其中:R是炔基; R 1是烷基,烯基,炔基,环烷基,环烷基 - 烷基,苯基和苯基烷基,所有后退基团依次可以携带一个或多个相同或不同的卤素原子; 烷氧基; 烯; 炔; 烷氧基; 卤代烷氧基; 烷; 卤代烷; alkysulfonyl; 甲酰基; 烷; 羟基; 卤素; 氰基; 硝基; 氨基; 烷基; 二烷基; 羧基; 烷; 链烯基氧基; 或炔氧基羰基; 并且n为0至3的整数,所述方法包括:(i)其中R,R 1和N 2如上定义的式(III)化合物的反应; m和m'独立地为0或1; 当m和m'均为0时,A为任选被一个或多个独立地选自卤素,羟基,烷氧基,C 1 -C 6烷氧基的烷基,烯基或炔基(适宜地具有至多8个碳原子) 4个二烷基氨基或氰基; 当m和m'中的一个是0而另一个是1时,A是含有至少两个碳原子(并且合适地具有至多8个碳原子)的烷二基,亚烯基或炔二基,任选被一个或多个独立选择的基团取代 卤素,羟基,烷氧基,C 1-4烷基氨基或氰基; 当m和m'均为1时,A是含有至少三个碳原子(并且合适地具有至多8个碳原子)的烷三基,亚烷基三炔或炔三基,任选地被一个或多个独立地选自卤素,羟基,烷氧基 C 1-4烷基氨基或氰基; 并且其中如果基团A含有三个或更多个碳原子,一个或多个碳原子可以各自任选被氧原子替代,条件是分子中任何两个氧原子之间至少有一个碳原子, 得到式(II)化合物,其中R,R 1和n如上所定义,和(ii)式(II)化合物与式 其中L是离去基团,得到如上文所定义的式(I)化合物。

    PROPARGYLETHER DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND THEIR USE FOR CONTROLLING PHYTOPATHOGENIC MICROORGANISMS
    3.
    发明申请
    PROPARGYLETHER DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND THEIR USE FOR CONTROLLING PHYTOPATHOGENIC MICROORGANISMS 审中-公开
    衍生物衍生物,其制备方法及其用于控制​​致病性微生物的用途

    公开(公告)号:WO2004033413A3

    公开(公告)日:2004-06-10

    申请号:PCT/EP0311218

    申请日:2003-10-09

    CPC classification number: A01N37/38 A01N41/02 A01N41/06 C07C243/32 C07C259/06

    Abstract: The invention relates to 4-propargyloxy-benzyl dervatives of the general formula (I ) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl or optionally substituted aryl; R2, R3, R5, R6, and R7 are each independently of each other hydrogen or optionally substituted alkyl; R4 is optionally substituted alkyl; X is O or N-R7; and R8 is a group R9 is optionally substituted aryl or optionally substituted heteroaryl; R10 and R11 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl; R12 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; R13 is hydrogen or optionally substituted alkyl, alkenyl or alkynyl; and R14 is optionally substituted alkyl or optionally substituted amino. These compounds possess useful plant protecting properties and may advantageously be employed in agricultural practice for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi.

    Abstract translation: 本发明涉及通式(I)的4-炔丙氧基 - 苄基衍生物,包括其旋光异构体和这些异构体的混合物,其中R 1是氢,任选取代的烷基,任选取代的环烷基或任选取代的芳基; R2,R3,R5,R6和R7各自独立地为氢或任选取代的烷基; R4是任选取代的烷基; X为O或N-R7; 并且R 8为基团R 9为任选取代的芳基或任选取代的杂芳基; R 10和R 11各自独立地为氢,任选取代的烷基,任选取代的烯基或任选取代的炔基; R12是任选取代的烷基,任选取代的环烷基,任选取代的芳基或任选取代的杂芳基; R13是氢或任选取代的烷基,烯基或炔基; 并且R 14是任选取代的烷基或任选取代的氨基。 这些化合物具有有用的植物保护性质,并且可有利地用于农业实践中以控制或防止植物病原微生物特别是真菌侵染植物。

    NOVEL N-P-PROPARGYLOXYPHENETHYL-THIOACETIC ACID AMIDES
    4.
    发明申请
    NOVEL N-P-PROPARGYLOXYPHENETHYL-THIOACETIC ACID AMIDES 审中-公开
    新型N-对 - 丙烯酰氧基苯乙酸 - 柠檬酸

    公开(公告)号:WO02081437A3

    公开(公告)日:2003-01-09

    申请号:PCT/EP0203623

    申请日:2002-04-02

    Abstract: The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alkynylsulfonyl or a group -O-CO-R11, -O-CO-O-R11 or -O-CO -CO-O-R11 wherein R11 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl. These compounds possess useful plant protecting properties and may advantageously be employed in agricultural practice for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi.

    Abstract translation: 本发明涉及通式(I)的N-炔丙氧基 - 苯乙基硫代乙酰胺衍生物,其包括其旋光异构体和这些异构体的混合物,其中R 1为氢,烷基,环烷基或任选取代的芳基,R 2和R 3各自独立地为 氢或烷基,R4是烷基,烯基或炔基,R5,R6,R7和R8各自独立地是氢或烷基,R9是氢,任选取代的烷基,任选取代的烯基或任选取代的炔基,R 10是任选取代的芳基或任选取代的 杂芳基,Z是羟基,任选取代的芳氧基,任选取代的烷氧基,任选取代的炔氧基,任选取代的芳硫基,任选取代的烷硫基,任选取代的炔硫基,任选取代的烷基亚磺酰基,任选取代的烯基亚磺酰基,任选取代的炔基亚磺酰基,任选取代的烷基磺酰基, ,选择 取代的炔基磺酰基或基团-O-CO-R11,-O-CO-O-R11或-O-CO-CO-O-R11,其中R11是氢,任选取代的烷基,任选取代的环烷基,任选取代的芳基或任选地 取代的杂芳基。 这些化合物具有有用的植物保护性质,并且可有利地用于农业实践中以控制或防止植物病原微生物特别是真菌侵染植物。

    PROCESS FOR THE PREPARATION OF AMINES
    6.
    发明申请
    PROCESS FOR THE PREPARATION OF AMINES 审中-公开
    制备氨基酸的方法

    公开(公告)号:WO2007068417A3

    公开(公告)日:2007-10-04

    申请号:PCT/EP2006011885

    申请日:2006-12-11

    Abstract: The present invention relates to a novel a process for the preparation of the compound of the general formula (I), wherein R 1 and R 2 are independently H or C 1-6 alkyl, which comprises treating with a reducing agent either a compound of the general formula (II), wherein R 1 and R 2 have the meanings given for the compound of the formula (I), R 3 is H or C 1-4 alkyl and Ph is phenyl, or a compound of the general formula (III), wherein R 1 , R 2 , R 3 and Ph have the meanings given for the compound of the formula (II), the reducing agent being effective to cleave the benzyl moiety Ph-CH(R 3 )- from the benzylamino moiety PhCH(R 3 )NH- in the compound of the formula (II) or in the compound of the formula (III) to leave an amino group and, in addition, in the case of the compound of the formula (III), to reduce both the 2,3-double bond and the double bond joining the R 1 R 2 C- moiety to the 9-position of the benzonorbornene ring to single bonds. It also relates to processes for the preparation of the compounds (II) and (III) and their precursors and to the compounds (II) and (III) themselves and certain of their precursors, which are novel compounds. The compounds (I) are useful for the preparation of various fungicidal heterocyclyl-carboxylic acid benzonorbornen-5-yl-amides.

    Abstract translation: 本发明涉及一种制备通式(I)化合物的新方法,其中R 1和R 2独立地为H或C 1 C-C部分到苯并降冰片烯环的9-位到单键。 它还涉及制备化合物(II)和(III)及其前体以及化合物(II)和(III)本身及其某些新型化合物的前体的方法。 化合物(I)可用于制备各种杀真菌性杂环基 - 羧酸苯并降冰片烯-5-基 - 酰胺。

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