| 摘要 |
<p>Prepn. of (17R)-7-alkyl-2'-oxo-spiro (androst-4-ene-17,5'- (1',2')-oxathiolan)-3-ones of formula (I'A) (where the 7-alkyl gp. has 1-4C atoms) comprises reaction of a 17 beta-hydroxy-21- tert. -butylsulphinyl-(17-alpha)-pregna- 4,6-diene-3-one, as a mixt. of diastereoisomers A and B or a single diastereoisomer, with an alkyl magnesium halide, alkyl-Mg-X, (where the alkyl has 1-4C atoms and X is halo) in the presence of a cuprous salt to give 17-beta-hydroxy-7-alkyl-21 -tertiarybutylsulphinyl (17-alpha)-pregn-4-ene-3-one, as a mixt. of the 7-alpha and 7-beta isomers; and opt. after sepn. of the isomers this cpd. is reacted with N-chloro- or N-bromo-succinimide to form (I'A). Aldosterone antagonisto which increase water and sodium diuresis whilst preserving organic potassium. The cpds. have little or no affinity for androgenic receptors and are free of androgenic or antiandrogenic side effects. They are mainly use to treat hypertension and arterial cardiac insufficiency. Typical adult oral dosage is 100 mg-1 g daily.</p> |
