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  • Title: Pictet-Spengler reactions for the synthesis of pharmaceutically relevant heterocycles.
    Author: Pulka K.
    Journal: Curr Opin Drug Discov Devel; 2010; 13(6):669-84. PubMed ID: 21061230.
    Abstract:
    The synthesis of biologically active heterocyclic scaffolds is one of the significant challenges of modern synthetic chemistry. The Pictet-Spengler (PS) reaction, known for approximately a century, remains a particularly popular cyclization method. This review describes recent applications of the PS reaction in the total synthesis of alkaloids and biologically active analogs of tetrahydroisoquinoline and tetrahydro-β-carboline. The utility of PS cyclization in the synthesis of a range of heterocyclic scaffolds is also described.
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