新化合物 A-失碳-17β-羟基-17α-乙炔基-Δ^(3(5),9(10))-雌甾二烯-2-酮的合成

SYNTHESIS OF A NEW COMPOUND: A NOR 17β HYDROXY 17α ETHYNYL Δ 3(5),9(10) ESTRA 2 ONE

报道新化合物Ａ失碳１７β羟基１７α乙炔基Δ３（５），９（１０）雌甾二烯２酮２的合成。文中探讨了用炔钾粗品对Ａ失碳Δ３（５），９（１０）雌甾二烯２，１７二酮１和Ａ失碳６β，１９环氧Δ３雄甾２，１７二酮３的选择性炔化，分别得标题化合物２（４４％）及Ａ失碳１７β羟基１７α乙炔基６β，１９环氧Δ３雄甾２酮４（６５％），４经还原性破开环氧、去羟甲基和去醋酰氧基合成了标题化合物２。四步总收率为３４％。

The article reports the synthesis of a new compound: A nor 17β hydroxy 17α ethynyl Δ 3(5),9(10) estra 2 one 2. The title compound was synthesized from A nor Δ 3(5),9(10) estra 2,17 dione 1 via direct selective ethynylation in 44% yield and from A nor 6β,19 oxido Δ 3(5),9(10) androst 2,17 dione 3 by a sequence of reaction including selective ethynylation, reductive deepoxidation, dehydroxymethylation, and deacetoxylation in 34% total yield.