Abstract:
The invention relates to 3'', 4''-anhydro- Beta , Ltalomethylosides of the general formula I
wherein R1 is methyl or formyl and R2 stands for Beta -H or Beta -OH, if there is no double bond in 4,5-position, and R3 is a butenolide or cumalin ring, a process for preparing them and their use in the treatment of cardiac and circulatory disturbances. The compounds are especially suitable for treating cardiac insufficiency, tachycardia and conduction defects.
Abstract:
Delta 14-20-KETO-21-DIALKOXY STEROIDS ARE PREPARED BY OXIDIZING 20-KETO-15 Alpha ,21-DIHYDROXY STEROIDS OF THE GENERAL FORMULA
IN WHICH Y is an oxo group which may be ketalized, a
GROUP WHICH MAY BE ETHERIFIED OR ESTERIFIED, A Delta 3-, Delta 2-, OR Delta 3,5-ENOL ETHER GROUP OR A Delta 3-, Delta 2-, OR Delta 3,5-ENAMINO GROUP, WHICH GROUPS MAY HAVE A DOUBLE BOND IN THE 4-POSITION, AND
IS A LOWER ACYCLIC OR CYCLIC ACETAL GROUPING, ACETALIZING THE 15 Alpha -HYDROXY-20-KETO-21-OXO STEROIDS OBTAINED, REACTING THE 15 Alpha -HYDROXY-20-KETO-21-DIALKOXY STEROIDS THUS OBTAINED WITH SULFONIC ACID HALIDES AND TREATING THE 15-SULFONIC ACID ESTERS THUS OBTAINED WITH AGENTS SPLITTING OFF ACIDS. The products are valuable intermediates for the manufacture of medicaments.
Abstract:
Process for the manufacture of 4-chloro-3-oxo-14 Beta -hydroxyor 4-chloro-3,14 Beta -dihydroxy-carda-4,20(22)dienolides wherein 3-oxo-carda-4,14,20(22)-trienolides are at first treated with chlorine, the compounds obtained are converted by hydrogenolysis into 3-oxo-4-chloro-carda-4,14,20-trienolides, these are treated with N-bromo-acid amides, and the 3-oxo-4chloro-14 Beta -hydroxy-15 Alpha -bromo-carda-4,20(22)-dienolides thus obtained are treated with Raney nickel and may be reduced.
Abstract:
21-(CYCLOBUTYL-CARBOXYLIC ACID)-ESTERS OF 3-OXO$4-STEROIDS USEFUL AS ANTI-INFLAMMATORY AGENTS, AND THEIR MANUFACTURE BY REACTION OF CYCLOBUTANE CARBOXYLIC ACID CHLORIDE WITH CORRESPONDING 21-HYDROXY-STEROIDS.
Abstract:
Cardioactive 3-amino-cardenolides and a method for preparing them by reacting a 3-oxo-cardenolide with hydroxylamine or its salts to form a cardenolide-3-oxime and then catalytically hydrogenating this intermediate.
AND METHODS OF MAKING THE SAME BY REACTING A STEROID ALCOHOL ROH, WITH A GLYCAL OF THE FORMULA
-CH2-O-R1 OR -CH(-O-R1)-CH2-O-R2
USEFUL FOR THE TREATMENT OF CARDIAC AND RENAL DISEASES, WHEREIN R IS A STEROID GROUP OF THE 3-HYDROXY-CARDENOLIDE OR 3-HYDROXYBUFADIENOLIDE SERIES, R1 IS ALIPHATIC OR AROMATIC ACYL, AND R2 IS HYDROGEN, METHYL, ETHYL, OR
Abstract:
A PROCESS FOR PREPARING 3B,14B-DIHYDROXY-CARA-4,20(22)-DIENOLIDES WHICH COMPRISES REDUCING 3-OXO-CARDA4,14,20(22)-TRIENOLIDES BY MEANS OF COMLEX METAL HYDRIDES TO THE CORRESPONDING 3B-HYDROXY-CARDA-4,14,20(22)-TRIENOLIDES; TREATING THESE COMPOUNDS WITH ACYLATING AGENTS; REACTING THE RESULTING 3B-ACYLOXY-CARDA-4,14, 20(22)-TRIENOLDIES WITH N-BROMO-ACYL AMIDES, AND CATALYTICALLY HYDROGENATING THE 4B-ACYLOXY-3B,14B-DIHYDROXY5A,15A-DIBROMO-CARD-20(22)-ENOLIDES SO OBTAINED IN THE PRESENCE OF A PRECIOUS METAL CATALYST AT A PH IN THE RANGE FROM 4.5 TO 7.5. THE PRODUCTS OF THE INVENTION ARE VALUABLE THERAPEUTICS FOR ORAL ADMINISTRATION IN DISEASES OF THE HEART AND CIRCULATION.