The organocatalytic alkylation of 2-methyl-N-heteroaromatics with alcohols has been achieved via S1-type C(sp)-H functionalization, providing a green and efficient synthesis of indole and ferrocene-functionalized N-heteroaromatics in high yields.
Structurally diverse amino acids and their ester derivatives were conveniently N,N′-dialkylated via TFE promoted cascade condensation/[1,5]-hydride transfer/cyclization for straightforward construction of tetrahydroquinazolines incorporating various amino acids.
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