NEW MATERIAL:A compound of formula I (X is H, halogen, hydroxyl; Y is H, lower alkyl, halogen, alkylthio; X and Y may incorporate to form a ring; Z1 is hydroxyl; Z2 is carboxyethyl alkali metal salt; Z1 and Z2 may incorporate together with the adjacent carbon atom to form the lactone ring of formula II; the dotted lines between C1WC2 as well as C6WC7 shows that double bonds may be there.
EXAMPLE: 17-Hydroxy-3-oxo-17α-pregna-4,11-diene-21-carboxylic acid γ-lactone.
USE: Antialdosterone agent.
PREPARATION: For example, in the presence of an acid catalyst, a compound of formula III is hydrolyzed to give a compound of formula IV, then the product is enolized to form a compound of formula V, then a reagent for transferring a methylene group is made to act on to give a compound of formula VI. Further, the product is allowed to react with a dialkyl malonate in the presence of a base and hydrolyzed with an alkali to give the objective compound of formula VII.
MATSUI TAKEAKI
HAGA NOBUHIRO
