Khripach V A, Zhabinskii V N, Tsavlovskii D N, Drachenova O A, Ivanova G V, Konstantinova O V, Zavadskaya M I, Lyakhov A S, Govorova A A, Groen M B, de Groot A
Institute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Kuprevich str., 5/2, 220141, Minsk, Belarus.
Steroids. 2001 Jul;66(7):569-79. doi: 10.1016/s0039-128x(00)00222-1.
A number of new steroidal 17-spirofuran derivatives of the 19-nor series containing Me, Et or (i)Pr-substituents in the heterocyclic moiety has been prepared, which are expected to have a strong progestagenic activity. The proposed approach made use of the 1-3-dipolar cycloaddition of low-molecular nitrile oxides with steroidal acetylenic alcohols followed by transformation of the isoxazole side chain.
已制备出多种19-去甲系列的新型甾体17-螺呋喃衍生物，其杂环部分含有甲基、乙基或异丙基取代基，预计具有较强的孕激素活性。所提出的方法是利用低分子腈氧化物与甾体炔醇的1,3-偶极环加成反应，然后进行异恶唑侧链的转化。
