Regioselective Synthesis of Thieno[3,2-b]quinolones by Acylation/Two-Fold Buchwald-Hartwig Reactions

A variety of thienoquinolones were synthesized from readily accessible thiophene derivatives by regioselective acylations and subsequent two-fold Buchwald-Hartwig-amination. This cyclization allows a convenient synthesis of biologically and pharmaceutically important thienoquinolones. Several thienoquinolones were synthesized in good to very good yields. The optical properties of the products were studied in detail.