FIELD: biotechnology.
SUBSTANCE: invention relates to biotechnology, organic chemistry and pharmaceutics, specifically to an improved method of producing 6-methylenecholest-4-en-3-one of formula I, having cytostatic activity. Method includes enzymatic selective oxidation of cholesterol II with formation of cholest-4-en-3-one III, its enolesterification with formation of 3-alkoxycholest-3,5-diene-3-one IV, condensation of IV with Mannich reagent, formed in situ from formaldehyde and secondary amine to form N,N-disubstituted derivative of 6-aminomethylcholest-4-en-3-one VI and deamination of compound VI with formation of 6-methylene group and obtaining target product. Synthesis steps are carried out without separation of intermediates.
EFFECT: providing a simple and effective method of producing a desired compound from cholesterol with a total output of not less than 84%.
15 cl, 1 tbl, 10 ex
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Authors
Dates
2025-06-02—Published
2024-11-26—Filed