2. Academic Validation
  3. Synthesis of benzo[c]quinolizin-3-ones: selective non-steroidal inhibitors of steroid 5 alpha-reductase 1

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

  • Bioorg Med Chem Lett. 1998 Oct 20;8(20):2871-6. doi: 10.1016/s0960-894x(98)00505-8.
A Guarna 1,  E G Occhiato,  D Scarpi,  R Tsai,  G Danza,  A Comerci,  R Mancina,  M Serio
Affiliations

Affiliation

  • 1 Dipartimento di Chimica Organica U. Schiff, CNR, Università di Firenze, Italy. [email protected]
PMID: 9873639 DOI: 10.1016/s0960-894x(98)00505-8
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 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.

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