Synthesis of benzo [c] quinolizin-3-ones: selective non-steroidal inhibitors of steroid 5α-reductase 1

…, G Danza, A Comerci, R Mancina, M Serio

Index: Guarna, Antonio; Occhiato, Ernesto G.; Scarpi, Dina; Tsai, Ruey; Danza, Giovanna; Comerci, Alessandra; Mancina, Rosa; Serio, Mario Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 20 p. 2871 - 2876

Full Text: HTML

Citation Number: 28

Abstract

A short and efficient synthesis of novel benzo [c] quinolizin-3-one derivatives is described. The synthesis is based on the tandem Mannich-Michael cyclization between 2-silyloxy-1, 3- butadienes and a Nt-Boc iminium ion. The prepared derivatives are selective inhibitors of human steroid 5α-reductase isoenzyme 1, thus having potential application as drugs for treatment of male pattern baldness and other DHT-dependent skin disorders.