METHOD OF SYNTHESIS OF 16α--METHYLATED STEROIDS Russian patent published in 1999 - IPC

FIELD: organic chemistry, steroids. SUBSTANCE: invention relates to a method of synthesis of 16α--methylated steroids of the formula (I) α- where cycles A and B are residue of the formula (a) or (b) where R - methyl or radical where -CH₂-OR′ - hydrogen atom or acyl-group; R′ and R₁ together form the second bond, or R₂ and R₁ together form epoxide at position R₂, or β - H, ketone group, R₁ - hydroxyl and α- - hydrogen atom, or R₂ - hydroxyl possibly substituted as ether or ester and R₁ - fluorine, bromine or methyl. Method of synthesis involves treatment of compound of the formula (II) R₂ where A, R, and R₁,R₂ have values indicated above with magnesium halogenide in the presence of copper diacetate or dipropionate followed by hydrolysis of the obtained 16R₃-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