Abstract

AbstractWe report an enzyme‐catalyzed dynamic kinetic resolution protocol for the one‐pot asymmetric synthesis of substituted purine derivatives. The controllable N‐9/N‐7 substitution, which posed formidable challenges in organic synthesis, could be accomplished by choosing different types of enzymes as catalysts. This method was proved scalable and was used to prepare a series of prodrugs of medicinally active acids. In addition, the recyclability test of the biocatalysts indicated the potential of this strategy for applications in the pharmaceutical industry.

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