（＋）16—苯氧基—17,18,19,20失四碳前列腺素F2α的合成

报道了一条简便合成标题化合物的路线，单羟基化合物（６）直接用二异丁基铝氢还原为ｒ－半缩醛，后者经Ｗｉｔｔｉｇ反应直接转化为目标物和１５－差向异构体。     

（＋）16－苯氧基－17，18，19，20失四碳前列腺素F2α的合成

报道了一条简便合成标题化合物的路线．单羟基化合物（６）直接￥用二异丁基铝氢还原为ｒ－半缩醛，后者经Ｗｉｔｉｇ反应直接转化为目标物和１５－差向异构体     

19—失碳—1α,25—二羟基维生素D3A环合成子的合成方法

综述了19-失碳-1α,25-二羟基维生素D3 A环合成子的合成方法,并分析和讨论了各方法的特点.     

（1‘R,2S,2’S）—2—（2—甲基—2—溴甲基—3—亚甲基）环戊基丙酸的合成

以商业易得的（＋）－内向３－溴莰酮－２为手性源合成了光学活性的（１’Ｒ,２Ｓ,２‘Ｓ）－２－（２－溴甲基－２－甲基－３－亚甲基）环戊基丙酸。     

2—（E）—芳亚甲基—5—环戊烯（1）基—5—烃基环戊酮类化合物的合成…

设计合成了含有αβ－不饱和酮和环戊烯基结构的２－（Ｅ）－芳亚甲基－５－环戊烯（１）基－５－烃基环戊酮类１１个未见文献报道的新化合物，初步药理结果显示。该类化合物ＥＡＣ和ＨｅｐＡ癌细胞具有较强的抑制作用，体内抑癌试验也显示一定活性，但抗炎活性较弱。     

Synthesis and biological activity of 17-esters of 6-dehydro-16-methylene-17 -hydroxyprogesterones

Synthesis and biological activity of 17-esters of 6-dehydro-16-methylene-17 alpha-hydroxyprogesterone are presented. A systematic study of the influence of the alteration of halogen at 6 and the acyl group at 17 on the progestational and antiandrogenic activities of the resulting structures is described. A convenient general method for synthesis of all of the members of the generic family from the precursors in common is described. It is believed that 6-chloro-16-methylene-17 alpha-hydroxy-4,6-pregnadiene 17-acetate, because of its structural similarity to chlormadinone acetate and its high progestational potency, will perform as a contraceptive at perhaps a lower dose than that of chlormadinone acetate.     

The pharmacological profile of TX 066 (17 alpha-acetoxy-6-methyl-19-nor-4,6-pregna-diene-3,20-dione), a new oral progestative

17 alpha-Acetoxy-6-methyl-19-nor-4,6-pregna-diene-3,20-dione (TX 066) has the pharmacological profile of a pure progestogen with no side effect such as androgenic activity. Its pituitary suppressing effect is relatively weak, as is also its antiestrogenic activity. It possesses a powerful antiandrogenic effect, which, in addition to the classic uses for progestogens, may make TX 066 useful in the treatment of certain diseases such as prostatic hypertrophy or the Stein-Leventhal syndrome.     

Antitumor activity of the new gestagen 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one

Antitumor activity of a new highly active promising gestagen 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one (butagest) was studied in mice with model cervical carcinoma (RShM-5). The reference drug was medroxyprogesteron acetate (MPA, Depo Provera) used in clinics. The new preparation introduced perorally in a dose of 1 mg per mice inhibited the model tumor growth by 73%, which was 18% (p < 0.01) more effective than the action of the reference drug MPA. The effect of the new gestagen was also studied in vitro with respect to human breast carcinoma of the MCF-7 line and human cervical carcinoma HeLa. The viability of the tumor cells was studied during a 6-day incubation with the drug at a concentration of 10(-7)-10(-5) M (MTT test). The reference compounds were progesterone and MPA. These drugs suppressed the growth of both MCF-7 and, in higher concentrations, of HeLa. Butagest inhibited the growth of HeLa in all concentrations. Thus, the new gestagen 17alpha-acetoxy-3beta-butanoyloxy-6-methyl-pregna-4,6-dien-20-one is capable of suppressing the viability of human breast carcinoma and human cervical carcinoma, being comparable or even more effective than the reference drugs.     

应用13C核磁共振INEPT方法测定5α-氯-16-次甲基-3β,6β,17α-三羟基-孕甾-20-酮-3β,17α二醋酸酯的结构

应用质子去偶及质子偶合INEPT方法测定药物合成中间体(Ⅱ)的结构。与宽带质子去偶及门控去偶方法比较,INEPT方法具有较高的灵敏度和选择性,节省实验时间。