| 摘要 |
<p>NEW MATERIAL:A compound expressed by formula I (R is ethyl or propyl). EXAMPLE:11beta,17alpha-Dihydroxy-21-chloro-pregn-4-ene-3,20-dione 17-butyrate. USE:A local anti-inflammatory agent. PROCESS:Hydrocortisone is dissolved in DMF and reacted with p-toluenesulfonyl chloride at room temperature to form 21-chlorohydrocortine, which is then reacted with trimethylchlorosilane to protect the hydroxyl group at the 11-position by trimethylsilylation. Butyric anhydride, benzene and p-toluenesulfonic acid are added and refluxed to acylate the 17-position, and the compound expressed by formula II (R' is acyl, nitro or trimethylsilyl) is obtained. The protecting group of the hydroxyl group at the 11-position is eliminated by mild hydrolysis with an acid to afford the compound of formula I.</p> |
