Process for the preparation of novel cardenolide and bufadienolide derivatives of ajmaline

Novel cardenolide and bufadienolide derivatives of ajmaline of the general formula in which R' represents -CH2-COR, where R denotes a 3-O-cardenolide or 3-O-bufadienolide residue, X represents halogen, R'' represents hydrogen, an azyl or alkyl radical, are obtained by reacting a corresponding cardenolide or bufadienolide with a mono-haloacetic acid halide in an organic solvent at a temperature of -10 to +25 DEG C, adding ajmaline to the resulting 3-O-haloacetyl derivative of cardenolide or bufadienolide in an organic solvent and subsequently isolating the end product. The novel ajmaline derivatives, which can be prepared in accordance with the invention, possess, for example, two actions which are of importance from the therapeutic point of view - the ability to relieve cardiac arrhythmia and to tonicise cardiac activity. They are used in medicine in general as active compounds in drugs for the treatment and prophylaxis of severe forms of cardiac diseases, such as myocardial infarction, arrhythmia, those which aggravate hypertension, cardiosclerosis, chronic cardiac insufficiency, rheumatism, infectious myocarditis, mitral insufficiency and a series of other severe and widespread diseases.