| 摘要 |
PURPOSE:To highly efficiently obtain in high yield the title compound useful as an aromatase inhibitor by a new method using, as starting material, a specific by-product formed in synthesizing the title compound from an androsten-dione by conventional method. CONSTITUTION:Firstly, 4-androsten-3,17-dione of formula I is converted to 14alpha- hydroxy-4-androsten-3,17-dione of formula II using microorganisms [pref. Acremonium strictum NN106(FERM P-9143)], and the ketone group at 3-site of the resultant compound is then alkoxylated. Thence, the resulting 3- alkoxy-14alpha-hydroxy-androsta-3,5-dien-17-one of formula III (R is chain alkyl) is oxidized with an oxidizing agent (pref. an aqueous solution of chromic anhydride-sulfuric acid) to obtain the objective compound of formula IV. The alkoxylation is made e.g. by the action of a combination of p-toluic acid and triethyl orthoformate. |
