| 摘要 |
<p>Steroids of formula (I) R = a 3-keto-DELTA4-, 3-keto-DELTA4,6-, 3-keto-DELTA1,4-, 3-keto-DELTA1,4,6-, 3-alkoxy-DELTA3,5-, 3-alkoxy-DELTA4,6-, 3-acyloxy-DELTA3,5-, 3-acyloxy-DELTA4,6-, 3-acyloxy-DELTA2,4,6- or 3-hydroxy-DELTA4,6-system. R' = H or acyl (I) have hormonal, esp. progestative, activity and in animal experiments have an effect on gonadotropin levels and display antiestrogenic activity; they can be used e.g. for regulating the menstrual cycle. (a) By treating (II) with a reducing agent: (b) By treating (III) with a chlorinating agent: (where R3 = a 3-acyloxy-DELTA3,5-, 3-alkoxy-DELTA3,5- or 3-keto-DELTA4,6-system). (c) (I; R' = H, R = 3-hydroxy-DELTA4,6) can be partially oxidised to (I; R' = H, R = 3-keto-DELTA4,6); (I; R = 3-keto-DELTA4 or 3-keto-DELTA4,6) can be dehydrogenated in at least one of the positions 1 (2) and 6(7); the 20-hydroxy group of (I; R' = H, R = 3-keto-DELTA4, 3-keto-DELTA1,4, 3-keto-DELTA4,6 or 3-keto-DELTA1,4,6) can be acylated; the acyloxy group of (I ; R' = acyl, R = 3-keto-DELTA4, 3-keto-DELTA1,4, 3-keto-DELTA4,6 or 3-keto-DELTA1,4,6) can be saponified; a free hydroxy group in (I; R = 3-hydroxy-DELTA4,6) can be acylated; the 3-hydroxy group in (I; R = 3-hydroxy-DELTA4,6) can be alkylated; (I; R = 3-keto-DELTA4) can be enol-etherified; and (I; R = 3-keto-DELTA4 or 3-keto-DELTA4,6) can be enolesterified.</p> |
