Efficient Synthesis of 21-Acetoxypregna-1,4,9(11),16-Tetraene-3,20-Dione, a Key Intermediate in the Synthesis of Highly Active Fluorinated Corticosteroids from 9α-Hydroxyandrostenedione

V. A. Andryushina; T. S. Stytsenko; N. V. Karpova; V. V. Yaderets; V. V. Dzhavakhiya

doi:10.1007/s11094-018-1898-y

Efficient Synthesis of 21-Acetoxypregna-1,4,9(11),16-Tetraene-3,20-Dione, a Key Intermediate in the Synthesis of Highly Active Fluorinated Corticosteroids from 9α-Hydroxyandrostenedione

Authors: Andryushina V.A.¹, Stytsenko T.S.¹, Karpova N.V.¹, Yaderets V.V.¹, Dzhavakhiya V.V.¹
Affiliations:
1. Federal Research Center Fundamentals of Biotechnology, Russian Academy of Sciences
Issue: Vol 52, No 9 (2018)
Pages: 776-780
Section: Drug Synthesis Methods and Manufacturing Technology
URL: https://journals.rcsi.science/0091-150X/article/view/245460
DOI: https://doi.org/10.1007/s11094-018-1898-y
ID: 245460

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Abstract

An efficient synthesis of 21-acetoxypregna-1,4,9(11),16-tetraene-3,20-dione, a key intermediate in the synthesis of highly active fluorinated corticosteroids from phytosterols, was developed. The method consisted of an original sequence of chemical and microbiological reactions and could be used to synthesize betamethasone, sinaflan, triamcinolone, and other fluorinated corticoids.