Synthesis of 2-alkyl-2-arylcyanoacetates via CuI/sodium picolinate-catalyzed direct arylation of α-substituted cyanoacetates

CuI/sodium picolinate-catalyzed direct arylation of α-substituted cyanoacetates takes place at 60 °C in the presence of Cs2CO3 and 4 Å molecular sieve, affording 2-alkyl-2-arylcyanoacetates in good to excellent yields. Both electron-rich and electronic-deficient aryl iodides, and some functionalized α-substituted cyanoacetates are compatible with the reaction conditions, thereby allowing diverse synthesis of 2-alkyl-2-arylcyanoacetates.