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    • 11. 发明授权
    • Method for preparing 1,3,4-substituted pyrazol compounds
    • 制备1,3,4-取代吡唑化合物的方法
    • US08598222B2
    • 2013-12-03
    • US12990340
    • 2009-05-04
    • Bernd WolfVolker MaywaldMichael KeilChristopher KoradinMichael RackThomas ZierkeMartin Sukopp
    • Bernd WolfVolker MaywaldMichael KeilChristopher KoradinMichael RackThomas ZierkeMartin Sukopp
    • A61K31/415C07D231/14
    • C07D409/12C07C251/76C07C251/84C07C251/86C07D231/14
    • The present invention relates to a process for preparing 1,3-substituted pyrazole compounds of the formula I in which X is especially a CX1X2X3 group in which X1, X2 and X3 are each independently especially hydrogen, fluorine or chlorine, R1 is C1-C4-alkyl or cyclopropyl, and R2 is hydrogen, CN or a CO2R2a group in which R2a is especially C1-C6-alkyl, comprising the following steps: i) reacting a compound of the formula II with a hydrazone of the formula III where the variables X and R2 in formula II are each as defined for formula I, Y is oxygen, an NRy1 group or an [NRy2Ry3]+Z− group, R3 is OR3a or an NR3bR3c group, and where the variable R1 in formula III is as defined for formula I, R4 and R5 are each independently hydrogen, C1-C6-alkyl, optionally substituted phenyl, where at least one of the R4 and R5 radicals is different from hydrogen, and where R4 and R5 together with the carbon atom to which they are bonded may also be a 5- to 10-membered saturated carbocycle; ii) treating the reaction product obtained with an acid in the presence of water.
    • 本发明涉及一种制备式I的1,3-取代吡唑化合物的方法,其中X特别是X 1,X 2和X 3各自独立地是氢,氟或氯,R 1是C 1 -C 4 - 烷基或环丙基,并且R 2是氢,CN或其中R 2a特别是C 1 -C 6 - 烷基的CO 2 R 2 a基团,包括以下步骤:i)使式II化合物与式III的腙反应,其中变量 式II中的X和R 2各自如式I所定义,Y是氧,NRy1基或[NRy2Ry3] + Z-基,R3是OR3a或NR3bR3c基团,其中式III中的变量R1如所定义 对于式I,R 4和R 5各自独立地为氢,C 1 -C 6 - 烷基,任选取代的苯基,其中R 4和R 5基团中的至少一个不同于氢,并且其中R 4和R 5与它们的碳原子一起 键也可以是5至10元饱和碳环; ii)在水存在下用酸处理反应产物。
    • 19. 发明申请
    • Method for production of aryl-substituted annelated pyrimidines
    • 芳基取代的环状嘧啶的制备方法
    • US20100087640A1
    • 2010-04-08
    • US12521877
    • 2008-01-10
    • Bernd WolfVolker MaywaldMichael KeilManuel BudichMichael RackManfred Ehresmann
    • Bernd WolfVolker MaywaldMichael KeilManuel BudichMichael RackManfred Ehresmann
    • C07D487/04
    • C07D487/04
    • The present invention relates to a process for preparing aryl-substituted fused pyrimidines of the general formula (I) in which L1 to L5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy etc.; Y1 to Y3 are C—RY or N; RY is H or optionally substituted C1-C4-alkyl or two adjacent RY together form a ring; X is OH, Cl or Br; which comprises (i) the reaction of a 2-phenylmalonate with a compound (III) or a tautomer thereof, in the presence of a suitable base, where the alcohol, released during the reaction, of the formula R—OH is continuously removed from the reaction mixture under reduced pressure; giving a compound of the formula (I) or a salt thereof in which X is OH, and, if X in the compounds of the general formula (I) is chlorine or bromine, (ii) the reaction of the compounds of the formula (I) obtained in step (i) or the salts with a halogenating agent.
    • 本发明涉及制备通式(I)的芳基取代的稠合嘧啶的方法,其中L 1至L 5为H,卤素,CN,NO 2,C 1 -C 4烷基,C 1 -C 4卤代烷基,C 1 -C 4 - 烷氧基,C1-C4-卤代烷氧基等; Y1至Y3为C-RY或N; RY为H或任选取代的C 1 -C 4烷基或两个相邻的RY一起形成环; X是OH,Cl或Br; 其包括(i)2-苯基丙二酸酯与化合物(III)或其互变异构体在合适的碱的存在下反应,其中反应期间释放的醇与式R-OH的连续从 减压下的反应混合物; 得到其中X是OH的式(I)化合物或其盐,并且如果通式(I)的化合物中的X是氯或溴,则(ii)式(I)化合物 I)或与卤化剂的盐。