NEW MATERIAL:A compound shown by the formula I (X is hydroxy, Y is alkali metallic salt of carboxyethyl, or X and Y together with neighboring carbon atom form lactone ring shown by the formula II).
EXAMPLE: 17-Hydroxy-6β-,7β-methylene-3-oxo-17α-pregna-1, 4, 11-triene-21-carboxylic acid.γ-lactone.
USE: A hypotensive diuretic. Useful for remedying hypertension, renal edema, etc.
PREPARATION: 3-17-Bis(ethylene dioxide)-androsta-5,11-diene as a starting raw material is deketalized, reacted with a secondary amine to give enamine shown by the formula III, which is processed into a compound shown by the formula IV, to give a halohydrin shown by the formula V. The compound shown by the formula V is processed into an allyl alcohol derivative, and converted into a silyl ether. Then, β-methylene group is introduced to the compound shown by the formula VI, the prepared silyl ether is processed into a hydroxyl compound, and oxidized, to give the desired substance.
MATSUI TAKEAKI
HAGA NOBUHIRO
