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    • 4. 发明申请
    • PROCESS FOR THE SYNTHESIS OF MANDIPROPAMID AND DERIVATIVES THEREOF
    • 合成麦芽苦苷及其衍生物的方法
    • WO2007020381A3
    • 2007-05-03
    • PCT/GB2006002946
    • 2006-08-08
    • SYNGENTA PARTICIPATIONS AGBOWDEN MARTIN CHARLESCLARK THOMAS AITCHESONGIORDANO FANNY DELPHINE BRIGTTJAU BEATSCHNEIDER HANS-DIETERSEIFERT GOTTFRIEDWISS JUERGZELLER MARTINFABER DOMINIK
    • BOWDEN MARTIN CHARLESCLARK THOMAS AITCHESONGIORDANO FANNY DELPHINE BRIGTTJAU BEATSCHNEIDER HANS-DIETERSEIFERT GOTTFRIEDWISS JUERGZELLER MARTINFABER DOMINIK
    • C07C231/02C07C33/46C07C43/174C07C43/313C07C59/70C07C69/734C07C213/02C07C231/12C07C235/34C07C251/16C07C255/37C07C315/04C07C317/46C07C319/20C07C323/62
    • C07C231/12C07C33/46C07C59/70C07C69/734C07C213/02C07C235/34C07C251/16C07C255/37C07C315/04C07C319/20C07C317/46C07C323/62
    • 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.
    • 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。