Guarna A, Occhiato E G, Scarpi D, Tsai R, Danza G, Comerci A, Mancina R, Serio M
Dipartimento di Chimica Organica U. Schiff, CNR, Università di Firenze, Italy.
Bioorg Med Chem Lett. 1998 Oct 20;8(20):2871-6. doi: 10.1016/s0960-894x(98)00505-8.
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 N-t-Boc iminium ion. The prepared derivatives are selective inhibitors of human steroid 5 alpha-reductase isoenzyme 1, thus having potential application as drugs for treatment of male pattern baldness and other DHT-dependent skin disorders.
