| 摘要 |
FIELD: organic chemistry, steroids. SUBSTANCE: invention relates to a method of synthesis of 16alpha--methylated steroids of the formula (I) alpha- where cycles A and B are residue of the formula (a) <EMI ID=0.578 HE=39 WI=48 TI=CHI> or (b) <EMI ID=0.579 HE=27 WI=33 TI=CHI> where R - methyl or radical <EMI ID=0.580 HE=27 WI=33 TI=CHI> where <EMI ID=0.581 HE=6 WI=15 TI=CHI> - hydrogen atom or acyl-group; <EMI ID=0.582 HE=3 WI=3 TI=CHI> and R<SB>1</SB> together form the second bond, or R<SB>2</SB> and R<SB>1</SB> together form epoxide at position R<SB>2</SB>, or beta - H, ketone group, R<SB>1</SB> - hydroxyl and alpha- - hydrogen atom, or R<SB>2</SB> - hydroxyl possibly substituted as ether or ester and R<SB>1</SB> - fluorine, bromine or methyl. Method of synthesis involves treatment of compound of the formula (II) R<SB>2</SB> where A, R, <EMI ID=0.583 HE=39 WI=39 TI=CHI> and R<SB>1</SB>,R<SB>2</SB> have values indicated above with magnesium halogenide in the presence of copper diacetate or dipropionate followed by hydrolysis of the obtained 16R<SB>3</SB>-methylated enolate with weak acid or buffer solution of weak acid pH value. Then synthesized enol is oxidized with per acid. EFFECT: proposed method does not require any intermediate substance isolation. 5 cl, 9 ex
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