首页> 外国专利> METHOD FOR OBTAINING STEROID DERIVATIVES 1 The invention relates to a new method for producing steroid derivatives having a hydrocarbon residue in the 17a position, saturated or unsaturated, substituted or unsubstituted, or a dicloalkyl radical, and having physiological activity. a prenatal radical, for example, compounds of 3-oxo-13p-ethyl-17a-ethynyl-17, p-oxygone — 4,9,11-triene, consisting in the fact that 3-ethylenedioxy-17-oxo-13 is prepared first 3-ethylgon- 4,9,1 i-triene which is reacted with an ethynylation reagent followed by hydrolysis of the ketal group at the 3 G7a-ethynyl derivative position. However, the ketalization of the 3-oxo group of the corresponding 3,17-dioxosteroid is not selective, with a low yield of the intermediate 3-ketal, which reduces the yield of the target product. In addition, in the known method, a 4,9,11-trienoic steroid with a closed ring A is used as a starting product, which can be obtained with the complete synthesis of a steroid only from an

METHOD FOR OBTAINING STEROID DERIVATIVES 1 The invention relates to a new method for producing steroid derivatives having a hydrocarbon residue in the 17a position, saturated or unsaturated, substituted or unsubstituted, or a dicloalkyl radical, and having physiological activity. a prenatal radical, for example, compounds of 3-oxo-13p-ethyl-17a-ethynyl-17, p-oxygone — 4,9,11-triene, consisting in the fact that 3-ethylenedioxy-17-oxo-13 is prepared first 3-ethylgon- 4,9,1 i-triene which is reacted with an ethynylation reagent followed by hydrolysis of the ketal group at the 3 G7a-ethynyl derivative position. However, the ketalization of the 3-oxo group of the corresponding 3,17-dioxosteroid is not selective, with a low yield of the intermediate 3-ketal, which reduces the yield of the target product. In addition, in the known method, a 4,9,11-trienoic steroid with a closed ring A is used as a starting product, which can be obtained with the complete synthesis of a steroid only from an

机译:获得类固醇衍生物的方法1本发明涉及一种新的制备类固醇衍生物的方法,该类固醇衍生物具有在17a位上的烃基,饱和或不饱和,取代或未取代的,或二氯烷基基团,并具有生理活性。产前自由基,例如3-oxo-13p-ethyl-17a-ethynyl-17,p-oxygone-4,9,11-triene的化合物,其特征在于3-乙烯二氧基-17-oxo-13是首先准备使3-乙基贡-4,9,1 i-三烯与乙炔化试剂反应,然后水解3 G7a-乙炔基衍生物位置的缩酮基。然而,相应的3,17-二氧代甾族化合物的3-氧代基的缩酮化不是选择性的,中间体3-缩酮的产率低,这降低了目标产物的产率。另外,在已知方法中,具有闭环A的4,9,11-三烯类固醇被用作起始产物,其可以仅通过从甲壳素完全合成类固醇来获得。

摘要

1355454 Steroids; 4,5-secosteroids ROUSSEL UCLAF 17 March 1972 [19 March 1971] 12579/72 Headings C2C and C2U The invention comprises compounds of Formulae III, IV and V and the preparation therefrom of steroids of Formula I (R is C 1-4 alkyl; and X is optionally substituted C 1-6 aliphatic hydrocarbyl, or C 3-6 cycloalkyl). The various conversions are effected with conventional reagents, the final step (V#I) being a base-induced cyclization.
机译:1355454类固醇; 4,5-secosteroids ROUSSEL UCLAF 1972年3月17日[1971年3月19日] 12579/72标题C2C和C2U本发明包含式III,IV和V的化合物以及由其制备的式I的甾类化合物(R为C 1-4烷基;和X是任选取代的C 1-6脂族烃基或C 3-6环烷基)。各种转化均采用常规试剂进行,最后一步(V#I)是碱基诱导的环化反应。

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