| 摘要 |
<p>FIELD: as steroidal agent. SUBSTANCE: product: present invention describes 20-oxo, 17alpha,, pregnane 21-dihydroxy derivatives of general formula I: <EMI ID=0.62 HE=33 WI=48 TI=CHI> wherein R<SB>1</SB> is H or CH<SB>3</SB>; R<SB>2</SB> is CH<SB>3</SB> or C<SB>2</SB>H<SB>5</SB>; cycles A, B, C and D include one or more double bonds in positions 1(2), 3(4), 4(5) or 9(11), or 3(4) and 5(6), or 4(5) and 6(7), or 1(2) and 4(5), or 1(2), 4(5) and 6(7), are substituted by one or more hydroxy functional groups, optionally protected in position 3,9 and/or 11 with one or two ketone functional group, optionally protected in position 3 and/or 11, with one or two fluorine, chlorine or bromine in position 6 and/or 99alpha, with one or more methyl or ethyl groups in positions 2,6 and 7, or and/or 16alpha or 16beta with one or two methoxy or ethoxy groups in position 3. Product is prepared by oxidation with peroxy acid of compound (II): <EMI ID=0.63 HE=33 WI=48 TI=CHI> wherein R<SB>1</SB>, R<SB>2</SB>, A, B, C and D are as defined above, in the presence of water in water-miscible solvent to give corresponding product (III): <EMI ID=0.64 HE=33 WI=54 TI=CHI> followed by solvolysis in acid or basic medium and optionally removed of protecting groups. EFFECT: more efficient preparation method. 16 cl1</p> |
