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    • 9. 发明申请
    • PROCESS FOR THE PREPARATION OF ARYL-PIRIDYL COMPOUNDS
    • 制备芳基 - 吡啶化合物的方法
    • WO2004037790A1
    • 2004-05-06
    • PCT/IT2002/000625
    • 2002-10-02
    • EUTICALS PRIME EUROPEAN THERAPEUTICALS SPAGIORDANO, ClaudioGIANNINI, Luca
    • GIORDANO, ClaudioGIANNINI, Luca
    • C07D213/48
    • C07D213/51C07D213/48
    • A method is described for the preparation of aryl-pyridine compounds of formula (I) by cross-coupling reaction, promoted by catalytic systems based on palladium or nickel between compounds of formula (II) and (III) in which: - Met represents Mg or Zn, - Y represents C1, Br, I or acetoxy, - Z represents I, Br, Cl, triflate, sulphonate, phosphate, - R l , R 2 , R 3 , R 4 , which are the same as one another or different, represent hydrogen, a linear and/or branched C l -C 4 alkyl, and/or an aryl, and/or a heteroaryl, or R l and R 2 and/or R 3 and R 4 , taken together, form a C 3 -C 8 ring, an aryl and/or a heteroaryl, - A represents -COR 5 where R 5 represents hydrogen, a linear and/or branched C l -C 4 alkyl, and/or an aryl, and/or a heteroaryl, or - A represents -CR s5 (OR 6 )(OR 7 ) where R 5 has the meaning described above and R 6 and R 7 , which are the same as one another or different, represent a linear and/or branched C 1 -C 4 alkyl, and/or an aryl, and/or a heteroaryl, or R 6 and R 7 , joined together, represent a C 1 -C 8 alkyl or alkenyl.
    • 描述了通过交叉偶联反应制备式(I)的芳基 - 吡啶化合物的方法,由式(II)和(III)化合物之间的基于钯或镍的催化体系促进,其中:Met表示Mg 或Zn,-Y表示C1,Br,I或乙酰氧基,-Z表示I,Br,Cl,三氟甲磺酸酯,磺酸酯,磷酸酯,-R1,R2,R3,R4彼此相同或不同,表示氢 ,线性和/或支链C 1 -C 4烷基和/或芳基,和/或杂芳基,或R 1和R 2和/或R 3和R 4一起形成C 3 -C 8环,芳基和/或 杂芳基,-A表示-COR 5,其中R 5表示氢,直链和/或支链C 1 -C 4烷基和/或芳基,和/或杂芳基,或-A表示-CR s(OR 6)(OR 7),其中R 5具有 上述含义和R 6和R 7彼此相同或不同,表示连接在一起的直链和/或支链C 1 -C 4烷基和/或芳基和/或杂芳基,或R 6和R 7 ,代表C1-C8 烷基或烯基。