Study on the synthesis of Exemestane

Abstract

Exemestane, a 3rᵈ-generation aromatase inhibitor, has been approved by FDA for the treatment of advanced breast cancer in postmenopausal women since 1995 and its patent was expired in 2015. Since the approval, Exemestane has been widely used in breast cancer patients and is shown to have good clinical effects. There are several published synthesis methods of Exemestane but there is not any such report in Viet Nam. Herein, we describe the two-step method for the synthesis of Exemestane from the commercial available compound, androst-4-ene-3,17-dione. The total yield of the synthesized Exemestane is 27.12 %. The structure of Exemestane and intermediate products were elucidated by MS and NMR spectroscopies.