PURPOSE: To obtain new safe compounds having low toxicities and useful for treating cardiac and vascular diseases such as heart failure and hypertension.
CONSTITUTION: There compounds of formula I [a wave line means that 17- positioned substituent can take α or β configuration; Y is O or guanidimino when a wave line at 3-position and a solid line are double bonded, or Y is OH, OR2 (R2 is H, a 2-6C alkyl or the like) or the like when the double line is a single bond; R is an aryl ring, or an (un)satd. heterocyclic ring contg. a hetero atom such as O and S; R1 is H, methyl or the like], their stereoisomers, metabolites and metabolite precursors such as 17β-phenyl-5α-androst-15- ene-3β,14β,17α-triol are obtained by reacting an aryl or heterocyclyl organic metal with a compd. of formula II (W is H or a protecting group; Y is Y in formula I other than guanidinoimino, and protected in the case of containing OH or the like) in an inert neutral solvent such as THF at -78°C to the room temperature.
RUIGI BERUNARUDEI
MARA FUERANDEI
MARUKO FURIGERIO
MARINA MAURO
RUIZA KUWADORI
