摘要:
Estrane and androstane derivatives of formula I ##STR1## wherein X is bromine, iodine, triphenyltin or trialkyltin of 1 to 6 carbon atoms per alkyl radical,Y represents two hydrogen atoms or methylene,Z represents two hydrogen atoms, oxo or alkylenedioxy of 2 to 6 carbon atoms andV is ethylene, vinylene, 1,3-propylene or cyclopropylene,R.sub.1 is hydrogen or a hydrocarbon radical of up to 8 hydrocarbon atoms, optionally interrupted by an oxa group or substituted by an oxo group,R.sub.2 is methyl or ethyl,R.sub.3 and R.sub.4 represent a carbon-carbon bond or R.sub.3 is hydrogen and R.sub.4 is hydrogen or methyl,.DELTA.symbolizes a 4(5)-double bond if Z signifies two hydrogen atoms or an oxo group; or a 5(6)-double bond or, for the estrane derivatives of formula I, also a 5(10)-double bond, if Z is alkylenedioxy,are pharmacologically effective substances or intermediates for preparation thereof.
摘要:
14,17.beta.-ethano-14.beta.-estratriene and estratetraene of Formula I ##STR1## wherein R.sup.1 is a hydrogen atom, a methyl or an acyl group of a monocarboxyclic acid of 1-12 carbon atoms,R.sup.2 is a hydrogen atom or an acyl group of a monocarboxylic acid of 1-12 carbon atoms,R.sup.3 is a hydrogen atom or a methyl group, and ##STR2## is a single or double C--C-bond show strong estrogenic activity.
摘要:
The disclosure relates to novel 1.alpha.,7.alpha.-dithio-substituted spirolactones of general Formula I ##STR1## wherein R.sup.1 is C.sub.1-3 -alkyl and C.sub.1-3 -acyl andR.sup.2 is hydrogen, C.sub.1-3 -alkyl and C.sub.1-3 -acyl,to their preparation, and to their use as medicinal agents.The compounds of this invention exhibit anti-aldosterone activity and show the profile of effectiveness of a pro-drug.
摘要:
6,6-ethylene-15,16-methylene-3-oxo-17.alpha.-pregn-4-ene-21,17.alpha.-carbolactones of general Formula I ##STR1## wherein ##STR2## is a CC-single of CC-double bond, R.sub.1 is a hydrogen atom or a methyl group,R.sub.2 is a methyl or ethyl group, and ##STR3## exhibit strong gestagen potency and an aldosterone-antagonistic activity.
摘要:
Androstane derivatives of Formula I ##STR1## wherein ---- is a single bond or a double bond,R.sub.1 is methyl or ethyl,R.sup.2 is hydrogen or alkyl of 1-8 carbon atoms,--X-- is --(CH.sub.2).sub.n --, --CH.dbd.CH(CH.sub.2).sub.m --, or --C.tbd.C--(CH.sub.2).sub.m --wherein n is 2 to 6 and m is 1 to 4,--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --CCl.dbd.CH--, ##STR2## --U--V
摘要:
A process for preparing a 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 steroid of the formula ##STR1## wherein Q is ##STR2## and R.sub.1 is hydrogen, trimethylacetyl, tert-butyldimethylsilyl, dimethyl-2-(3-methylbutyl)silyl or tribenzylsilyl,comprises fermenting a 3.beta.-hydroxy-.DELTA..sup.5 -steroid of the formula ##STR3## wherein Q is as defined above, andR.sub.2 is hydrogen or alkanoyl of 2-6 carbon atoms,with a culture of Botryodiplodia malorum to obtain the corresponding 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid; and, optionally, reacting the resultant product with trimethylacetic anhydride, tert-butyldimethylsilyl chloride, dimethyl-2-(3-methylbutyl)silyl chloride, or tribenzylsilyl chloride.
摘要:
3-Deoxy-.DELTA..sup.15 -steroids of the formula ##STR1## wherein R.sup.1 is hydrogen or an acyl group of a C.sub.1-15 hydrocarbon carboxylic acid, andR.sup.2 is ethynyl, chloroethynyl or propynyl are valuable progestationally effective compounds having low attendant androgenic side effects.
摘要:
A process for preparing an 11.beta.-hydroxy steroid of the formula ##STR1## wherein represents a single bond or a double bond;X is hydrogen, fluorine, chlorine or methyl; andV is methylene, ethylene, ethylidene or vinylidene;comprises fermenting an 11-deoxy steroid of the formula ##STR2## wherein , X and V are as defined above,R.sub.1 is hydrogen or C.sub.1-6 -alkyl; andR.sub.2 is C.sub.1-6 -alkyl;with a fungal culture of a genus Curvularia.
摘要:
A process for the preparation of pregnane derivatives of the formula ##STR1## wherein R.sub.1 is methyl or ethyl and R.sub.2 is methyl, ethyl, formyl, or acetyl, comprises reacting a nitrate ester of the formula ##STR2## wherein R.sub.1 is as above, in the presence of a catalytic amount of a mercury salt of a lower carboxylic acid with formic acid or acetic acid in a dipolar aprotic or basic solvent or with methanol or ethanol in an aprotonic, especially water-miscible, solvent in the presence of a mineral acid.
摘要:
20-Cyano-17.alpha.-H steroids having as the 17-position substituent the group ##EQU1## wherein R is H, alkyl of 1-8 carbon atoms or benzyl, having a 13-methyl or 13-ethyl group and which are unsubstituted or substituted with an .alpha.-methyl group in the 16-position are converted to the corresponding 20-keto steroids by reaction in an aprotic solvent with a deprotonating agent containing an alkali metal, an alkaline earth metal, copper(I) or thallium(I), and optionally additionally with a copper(I) salt or a thallium(I) salt or a silver(I) salt, and thereafter conducting an oxidative splitting reaction with oxygen. The thus-produced 17.beta.-oxalyl steroids possess pharmacological activity, e.g., anti-inflammatory activity, or are useful as intermediates for the production of pharmacologically active steroids.