作者:Ulf Wellmar、Anna-Britta Hömfeldt、Salo Gronowitz
DOI:10.1002/jhet.5570330232
日期:1996.3
Pd(0)-catalysed coupling between arylboronic acids and aryl bromides or iodides in weakly alkaline medium has been used for the preparation of 5-(3′-chlorophenyl)-, 5-(3′-iodophenyl)-, 5-(3′-aminophenyl)-, 5-(3′-azidophenyl)-, 5-(3′-methylthiophenyl)- and 5-(3′-styryl)-substituted 2,4-di-t-butoxypyrimidines. In the coupling between 2,4 di-t-butoxy-5-pyrimidineboronic acid and the six different aryl
在弱碱性介质中芳烃硼酸与芳基溴化物或碘化物之间的Suzuki Pd(0)催化偶联已用于制备5-(3'-氯苯基)-,5-(3'-碘苯基)-,5- (3'-氨基苯基) - ,5-(3'-叠氮基苯基) - ,5-(3'-甲硫基苯基) -和5-(3'-苯乙烯基)取代的2,4-二-吨-butoxypyrimidines。在2,4-二-之间的耦合吨丁氧基-5-嘧啶硼酸和用作偶联伴侣,所述六个不同的芳基卤,只有1-叠氮基-3-溴苯没有给出令人满意的产率,18%。其他五个芳基卤化物以41-92%的收率得到了所需的5-(3'-取代苯基)-2,4-二-r-丁氧基嘧啶。这五个5-(3'-取代的苯基)的脱烷基化-2,4-二吨-butoxypyrimidines在2.5中号盐酸以几乎定量的产率得到相应的5-(溴芳基)尿嘧啶。由5-(3'-氨基苯基)-2,4-二-r-丁氧基嘧啶直接以43%的产率制备5-(3'-叠氮苯基)尿嘧啶。