首页> 外国专利> Improed process for coupling arylboronic acids with aryl halides - carried out in presence of a transition metal (esp. palladium) catalyst with a bidentate, lipophilic, aliphatic phosphine ligand

Improed process for coupling arylboronic acids with aryl halides - carried out in presence of a transition metal (esp. palladium) catalyst with a bidentate, lipophilic, aliphatic phosphine ligand

机译:芳基硼酸与芳基卤化物偶联的改进方法-在过渡金属(尤其是钯)催化剂与双齿,亲脂性,脂肪族膦配体的存在下进行

摘要

An improved method for carrying out a cross-coupling reaction comprises performing the reaction in the presence of a transition metal catalyst contg. a lipophilic, aliphatic phosphine ligand of formula (R1)2-P-R2 (I) or also a gp. of formula -R3-P(R1)2 (II) R1 = 1-6C alkylor alkoxy, or 4-8C cycloalkyl or cycloalkoxy, pref. 3-6C alkyl, 3-6C alkoxy or cyclohexyl; R2 = as for R1; R3 = 1-20C alkylene. Also claimed is a process for the prodn. of bis-aryl cpds. (III) in the presence of a catalyst contg. (I). Also claimed is 2,6-difluoro-4-chloro-trifluoromethoxy-benzene (VI). USE/ADVANTAGE - The process provides an improved method for carrying out the above coupling reaction, which can be performed on a large scale with little risk and low cost, esp. for the prodn. of F-substd. biphenyl derivs. with mesogenic gps., using (VI) as coupling component. The process is carried out at readily accessible temps. from readily available starting materials, and gives (III) in high yield (contrast conventional coupling catalysts).
机译:进行交叉偶联反应的改进方法包括在包含过渡金属催化剂的情况下进行反应。式(R1)2-P-R2(I)的亲脂性脂族膦配体或gp。式-R 3 -P(R 1)2的通式(II)R 1 = 1-6C烷基或烷氧基,或4-8C环烷基或环烷氧基,优选。 3-6C烷基,3-6C烷氧基或环己基; R2 =与R1相同; R 3 = 1-20C亚烷基。还要求保护一种产品的方法。双芳基cpds。 (III)在催化剂续存在下。 (一世)。还要求保护的是2,6-二氟-4-氯-三氟甲氧基-苯(VI)。使用/优点-该方法提供了进行上述偶联反应的改进方法,该方法可以大规模进行,风险小,成本低,尤其是。为产品F-substd。联苯衍生物。使用(VI)作为耦合成分的介晶gps。该过程在容易获得的温度下进行。由容易获得的起始原料制得,并以高收率得到(Ⅲ)(与常规偶合催化剂相比)。

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