Convenient synthesis of 2,4-disubstituted pyrido[2,3-d]pyrimidines via regioselective palladium-catalyzed reactions
作者:Yassine Riadi、Stephane Massip、Jean-Michel Leger、Christian Jarry、Saïd Lazar、Gérald Guillaumet
DOI:10.1016/j.tet.2012.04.051
日期:2012.6
A novel and effective route for the synthesis of 2,4-disubstituted pyrido[2,3-d]pyrimidines III is reported starting from the corresponding 2,4-dichloropyridopyrimidine 1 through regioselective functionalization palladium-catalyzed C–C coupling reactions, by two successive palladium-catalyzed reactions involving an original regioselective chlorine discrimination. Alternatively, type III compounds were
据报道,从相应的2,4-二氯吡啶并嘧啶1开始,通过区域选择性官能化钯催化的CC偶联反应,合成了2,4-二取代的吡啶并[2,3- d ]嘧啶III的新颖有效途径。连续的钯催化反应,涉及原始的区域选择性氯鉴别。或者,通过C-2氯从2进一步修饰III型化合物,进一步取代用作临时C-4保护基的C-4异丙基硫烷基。进一步的Suzuki-Miyaura交叉偶联反应导致C-2和C-4双取代的化合物。