Formestane, 4-Hydroxyandrostenedione, CGP-32349, 4-OHA, Lentaron Depot, Lentaron

4-雄烯-4-醇-3,17-二酮Chemical Name: 4-Hydroxyandrost-4-ene-3,17-dione
CAS No. 566-48-3
项目整合开发状态: Launched-1992
项目研究机构: Novartis (Originator), Kyorin (Licensee)
合成路线:A novel synthetic strategy for the preparation of formestane has been published:The oxidation of 5alpha-3-androsten-17-one (I) with H2O2 in formic acid gives the epoxide (II),which,without isolation,yields 3alpha,4beta-dihydroxy-5alpha-androstan-17-one (III).The reaction of (III) with DMSO and trifluoroacetic anhydride (TFAA),and then with triethylamine affords 3-hydroxy-5alpha-2-androstene-4,17-dione (IV),which is finally submitted to basic isomerization catalyzed by sodium methoxide