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  • Title: Convergent synthesis of the quinolone substructure of BILN 2061 via carbonylative Sonogashira coupling/cyclization.
    Author: Haddad N, Tan J, Farina V.
    Journal: J Org Chem; 2006 Jun 23; 71(13):5031-4. PubMed ID: 16776542.
    Abstract:
    A convergent synthesis of quinolone 2 (key substructure of the protease inhibitor BILN 2061) was developed via palladium-catalyzed carbonylation of 2-iodo-5-methoxyaniline (4) with thiazolylacetylene 5.
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