[EN] PROCESS FOR THE PREPARATION OF PYRIDYL-ARYL-SULPHONIC COMPOUNDS<br/>[FR] PROCEDE POUR LA PREPARATION DE COMPOSES SULFONIQUES DE PYRIDYLE-ARYLE
申请人:EUTICALS PRIME EUROP THERAPEUT
公开号:WO2004039779A1
公开(公告)日:2004-05-13
A method is described for the preparation of pyridyl-aryl-sulphonic compounds of formula (I), by cross-coupling reaction, promoted by catalytic systems based on palladium or nickel between compounds of formulae (II, III), in which; a) Met represents Mg or Zn, b) Y represents C1, Br, I or acetoxy, c) Z represents I, Br, Cl, triflate, sulphonate and/or sulphone, d) R1, R2, R4, R5, which are the same as one another or different, represent H, a linear and/or branched C1-C4 alkyl, and/or an aryl, and/or a heteroaryl, or R1 and R2 and/or R4 and R5, taken together, form a heteroaryl, and e) R3 represents a linear, branched or cyclic C1-C8 alkyl and/or an aryl, and/or a heteroaryl.
本文描述了一种制备式(I)吡啶基-芳基-磺酸化合物的方法,通过钯或镍基催化体系促进式(II,III)化合物之间的交叉偶联反应,其中:a)Met代表Mg或Zn,b)Y代表C1,Br,I或乙酰氧基,c)Z代表I,Br,Cl,三氟甲磺酸盐,磺酸盐和/或磺酰基,d)R1,R2,R4,R5相同或不同,代表H,线性和/或支链C1-C4烷基,和/或芳基,和/或杂芳基,或R1和R2和/或R4和R5一起形成杂芳基,e)R3代表线性,支链或环状C1-C8烷基和/或芳基和/或杂芳基。