摘要
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.
出处
《药学学报》
CAS
CSCD
北大核心
1997年第6期416-419,共4页
Acta Pharmaceutica Sinica
关键词
避孕药
失碳
炔诺酮
雌甾二烯酮
羟基
合成
A nor 17β hydroxyl 17α ethynyl Δ
3(5)
9(10)
estra 2 one
Selective ethynylation
Reductive deepoxidation
Dehydroxymethylation
Deacetoxylation
Financial support of this work was provided by the National Committee of Family Planning an