PURPOSE: To obtain a new compd. which is useful as a therapeutic drug for cardiovascular diseases such as heart failure and hypertension, is low toxic and which acts as a partial agonist for enzymic activity of Na+, K+-ATPase.
CONSTITUTION: This compd. is expressed by formula I (double lines of dotted lines and solid lines represent single bonds or double bonds; X is S, O; R is a 2-6C alkyl, a 3-6C alkenyl, alkynyl or the like), for example, 3β-(2-(trimethylammonium)ethoxy)-14β-hydroxy-5β-carbo-20(22)-enolidechloride. The compd. is obtd. by condensation of a compd. expressed by formula II with a compd. expressed by R-Y (Y is an electron attractive group). The condensation reaction is preferably carried out in an inert aprotic solvent such as THF in the presence of a strong base such as hydrogenated sodium at -20 to 110°C. The compd. expressed by formula I is preferably purified by flush chromatography on a silica gel.
RUIJI BERUNARUDEI
PATORITSUIA FUERAARI
MAURO GOBIINI
MARUKO TORI
ROREDANA BUARENTEINO