(17R)-Spiro- androstane-17,1'-cyclobutan!-2'-ones, methods for their manufacture and intermediates useful therein

摘要

(17R)-Spiro- androstane-17,1'-cyclobutan!-2'-ones are prepared by the reaction of a 17-oxo androstane, wherein all other ketones are blocked, with a cyclopropylarylsulfide or with a cyclopropylarylsulfonium salt having a non-nucleophilic anion, in an organic solvent together with a strong base, followed by reaction in situ of the intermediate thereby formed with aqueous acid or water.PP Some (17R)-spiro- androstan-17,1'-cyclobutan!-2'-ones are useful as intermediates in preparing (17R)-spiro- 3-oxo-4-androstene-17,1'-cyclobutan!-2'-ones which are aldosterone antagonists. Additionally, (17R)-spiro- androstane-17,1'- cyclobutan!-2'-ones are useful as intermediates in preparing known 17. alpha.-pregnane-21,17&bgr;-carbolactones, valuable aldosterone blocking agents.