(20S)-20-羟基胆甾烷-3,16-二酮的合成

The Synthesis of(20S)-20-Hydroxycholestane-3,16-Dione

以妊娠双烯醇酮醋酸酯为起始原料,经过7步反应以13.1%的总收率合成了一个具有抗4种肿瘤细胞(ED50=1μg/mL)的海洋天然产物(20S)-20-羟基胆甾烷-3,16-二酮.关键反应为底物控制的不对称杂原子共轭加成反应.

The synthesis of （20S）-20-hydroxycholestane-3,16-dione, a marine natural product against four tumor cell lines （ED50= 1 μg/mL）, was achieved from 16-dehydropregnenolone acetate in seven steps with a 13.1% overall yield. The key step was a substrate controlled asymmetric heteroatom conjugated addition.