Tetrahedron Letters p. 9403 - 9406 (1996)
Update date:2022-08-04
Topics:
Michael, Joseph P.
De Koning, Charles B.
Stanbury, Trevor V.
A simple synthesis of tricyclic analogues of the quinolone antibiotics bearing a diverse range of substituents on the aromatic ring is described. The key steps involve unprecedented Reformatsky reaction between diethyl bromomalonate and N-arylpyrrolidine-2-thiones 8, followed by cyclisation of the resulting enaminone intermediates 9 in polyphosphoric acid.
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Doi:10.1021/jo00292a041
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