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    • 31. 发明授权
    • Fluorine-containing diphenyl acrylamide antimicrobial agents
    • 含氟二苯基丙烯酰胺抗菌剂
    • US6020332A
    • 2000-02-01
    • US20333
    • 1998-02-09
    • Zongcheng LiChangling LiuWucheng Liu
    • Zongcheng LiChangling LiuWucheng Liu
    • A01N37/38C07D295/185A01N43/84C07D265/30
    • C07D295/185A01N37/38
    • Fluorine-containing diphenyl acrylamide of general formula (I) have antimicrobial properties. wherein R.sub.1 and R.sub.2 are independently selected from (C.sub.1 -C.sub.6)alkyl group, alkyl group, (C.sub.1 -C.sub.6)alkoxy group, halo(C.sub.1 -C.sub.6)alkyl group, halo(C.sub.1 -C.sub.6)alkoxy group, (C.sub.1 -C.sub.6)alkoxy(C.sub.1 -C.sub.6)alkyl group, (C.sub.3 -C.sub.6)cycloalkyl group, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl group, (C.sub.2 -C.sub.6)alkenyl group, halo(C.sub.2 -C.sub.6)alkenyl group, (C.sub.3 -C.sub.6)alkynyl group, halo(C.sub.3 -C.sub.6)alkynyl group, aryl group, aryloxy(C.sub.1 -C.sub.12)alkyl group, aralkyl group, heterocyclic group;or R.sub.1 and R.sub.2 when taken together may form a 5 or 6-membered ring such that;when R.sub.1 and R.sub.2 are in a 5 membered ring R.sub.1 and R.sub.2 taken together is C(R.sub.6 R.sub.7); andwhen R.sub.1 and R.sub.2 are in a 6 membered ring R.sub.1 and R.sub.2 taken together is CHR.sub.6 -CHR.sub.7 ;where R.sub.6 and R.sub.7 are independently selected from hydrogen, (C.sub.1 -C.sub.6)alkyl group or halogen.
    • 具有通式(I)的含氟二苯基丙烯酰胺具有抗微生物性质。 其中R1和R2独立地选自(C1-C6)烷基,烷基,(C1-C6)烷氧基,卤代(C1-C6)烷基,卤代(C1-C6)烷氧基,(C1-C6) 烷氧基(C1-C6)烷基,(C3-C6)环烷基,(C3-C6)环烷基(C1-C4)烷基,(C2-C6)烯基,卤代(C2-C6)烯基,(C3 -C 6)炔基,卤代(C 3 -C 6)炔基,芳基,芳氧基(C 1 -C 12)烷基,芳烷基,杂环基; 当R 1和R 2一起时可以形成5或6元环,使得 当R 1和R 2为5元环时,R 1和R 2一起为C(R 6 R 7); 当R1和R2为6元环时,R1和R2一起为CHR6-CHR7; 其中R 6和R 7独立地选自氢,(C 1 -C 6)烷基或卤素。
    • 38. 发明授权
    • Preparation method of phenylcarboxamides
    • 苯甲酰胺的制备方法
    • US08217179B2
    • 2012-07-10
    • US12918133
    • 2009-03-30
    • Bin LiHongfei WuHaibo YuHuibin Yang
    • Bin LiHongfei WuHaibo YuHuibin Yang
    • C07D401/04
    • C07D401/04
    • A preparation method of phenylcarboxamides of formula (I), the reaction scheme of which is as follows: wherein the groups are defined in the description. In this method, 3-halo-1-(3-chloro-2-pyridinyl)-4,5-dihydro-1H-pyrazole-5-carboxylic acid esters (V) as the raw materials are hydrolyzed to obtain carboxylic acids of formula (IV) under a basic condition, and carboxylic acids (IV) are simultaneously acyl halogenated and oxidated to get acyl halide of formula (III), and then without the presence of a acid binging agent, acyl chlorides (III) are reacted with substituted anilines (II) to get phenylcarboxamides of formula (I) in high yield.
    • 式(I)的苯甲酰胺的制备方法,其反应方案如下:其中这些基团在说明书中定义。 在该方法中,将作为原料的3-卤代-1-(3-氯-2-吡啶基)-4,5-二氢-1H-吡唑-5-羧酸酯(V)水解,得到式 (Ⅳ),羧酸(Ⅳ)同时进行酰基卤化和氧化,得到式(Ⅳ)的酰卤,然后不存在酸性起始剂,酰基氯(III)与取代的 苯胺(II)以高产率得到式(I)的苯基甲酰胺。