Abstract:
A METHOD FOR SYNTHESIZING ESTERS IN WHICH THE ACID MOIETY IS THAT OF A HYDROXY ACID AND THE ALCOHOL MOIETY IS A 3-HYDROXY-CARDENOLIDE OR 3-HYDOXY-BUFADIENOLIDE, BY ESTERIFYING THE STEROL WITH AN ACID ANHYDRIDE OR AN ACID CHLORIDE OF THE HYDROXY ACID, THE HYDROXY GROUPS OF WHICH HAVE BEEN ACETALIZED OR KETALIZED, AND THEN SELECTIVELY REMOVING SAID ACETAL OR KETAL GROUPS BY ACID HYDROLYSIS. CARDI-ACTIVE OXY-ESTERS PRODUCED BY THIS METHOD.
Abstract:
MANUFACTURE OF 3B-HYDROXY-5B-CARDENOLIDES OF THE 14DEHYDRO OR 14B SERIES BY TREATMENT OF 3-DETO-5B-CARDENOLIDES WITH IRIDIUM (IV)-HYDROCHLORIC ACID, ITS SALTS OR IRIDIUM (III)-CHLORIDE IN THE PRESENCE OF TRIALKYL-PHOSPHITE.
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.