首页> 外国专利> MEDICINE USED IN CASE OF TREATING MISCARRIED FETUS,DISFUNCTION OF OVARY AND HYPERPLASIA OF ENDOMETRIUM

MEDICINE USED IN CASE OF TREATING MISCARRIED FETUS,DISFUNCTION OF OVARY AND HYPERPLASIA OF ENDOMETRIUM

机译:用于治疗输精管畸形,卵巢功能异常和子宫内膜增生的药物

摘要

6 alpha-Methyl-cyclohexano 1',2',16 alpha, 17 alpha pregn-4-ene-3, 20-dione (I) is prepd by reacting cyclohexano 1',2',-16 alpha, 17 alpha pregn-5-en-3beta-alpha-20-one-3-acetate (IIe withperacid in a polar org. solvent; heating the resulting cyclohexano 1', 2', 16 alpha, 17 alpha 5 alpha,6 alpha-epoxy-pregnan-3 beta-ol-20-one 3-acetate (III) with CH3MgI in an org. solvent with heating to 100 degrees C; oxidising the resulting 6beta-methyl-cyclohexano 1',2'-16alpha, 17alpha-pregnane-3beta,5alpha-diol-20-one (IV) with chromium trioxide and H2SO4 in acetone, dehydrating the resulting 3-keto-5alpha-hydroxy-6beta-methyl deriv. (V) with HCl in acetic acid; and isolating (I). (I) has progestagenic activity and can be used as active substance in a hormonal contraceptive (more active then e.g. mestranol). It can also be used for treating functional insufficiency of the corpus luteum (sterility, premature birth etc).
机译:通过使环己酮1',2',-16 alpha,17 alpha pregn--制备6α-甲基-环己酮1',2',16 alpha,17 alpha pregn-4-ene-3,20-dione(I) 5-en-3beta-alpha-20-one-3-acetate(IIe与过酸在极性有机溶剂中;加热所得环己基1',2',16 alpha,17 alpha 5 alpha,6 alpha-epoxy-pregnan-在加热至100摄氏度的条件下,在有机溶剂中与CH3MgI合并成3β-ol-20-one3-乙酸盐(III);将所得的6beta-甲基-环己酮1',2'-16alpha,17alpha-pregnane-3beta,氧化,用三氧化铬和H2SO4在丙酮中的5alpha-diol-20-one(IV),在乙酸中的HCl脱水生成的3-keto-5α-羟基-6beta-甲基衍生物(V);然后分离(I)。 I)具有孕激素活性,可以用作激素避孕药的活性物质(比甲羟雌醇更活泼),也可以用于治疗黄体功能不全(不育,早产等)。

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