A mild and selective C6 arylation strategy for pyrrolo[2,3-d]pyrimidine derivatives with arylboronic acids at room
temperature is described. This unified protocol has been achieved
by the synergistic combination of Pd(II)/TEMPO catalysis and CF3CO2H promotion under silver-, base-, and additive-free
conditions. The broad substrate scope, good functional group tolerance,
excellent regioselectivity, and air and moisture tolerant conditions
make this process attractive for the effective synthesis and modification
of targeted small molecule drugs.
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