QUY TRÌNH HIỆU QUẢ TỔNG HỢP PREGNA-4-EN-17α, 21-DIOL-3,20-DION TỪ ANDROSTENDION ỨNG DỤNG PHƯƠNG PHÁP ACETYLEN

Summary

Vietnam currently imports the pharmaceutical compounds up to 90 %, in particular 100 % of steroidal drugs. Currently, industrial production is based on the chemical syntheses of corticosteroids from either 16-dehydropregnenolone acetate (obtained from diosgenin, solasodin) or androstenedione (obtained from phytosterols). The development of shorter synthetic schemes and more economically feasible technologies is of great significance.

In this paper, we present an efficient procedure for the synthesis of the pregna-4-ene-17α,21-diol3,20-dione (Reichsteine‘s Substance S) in total yield more than 53 %, a key intermediate for synthesis of corticoids such as hydrocortisone and prednisolone as well as betamethasone, etc., from androstenedione, which is a product of a bio-oxidative degradation of the side chain of phytosterols.

The strusture of the product and its intermediates was examined by physical methods such as: IR, MS, ¹H and ¹³C-NMR.

Keywords: Pregna-4-ene-17α,21-diol-3,20-dione (Reichsteine’ s Substance S), androstenedione. 

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