6-alkoxy - 16 - alkylidene - 17alpha - lower alkanoyloxy-21-desoxy - 4 6 - pregnadienes methods for their manufacture and intermediates produced thereby
Abstract
Abstract 6-ALKOXY-16-LOWER ALKYLIDENE-17A-LOWER ALKANOYLOXY4,6-PREGNADIENE-3,20-DIONES AND 1A,2A-CYCLOMETHYLENE DERIVATIVES THEREOF HAVING PROGESTATIONAL AND ANTI-ANDROGENIC ACTIVITY ARE PREPARED BY TREATING A 6-KETO-16-LOWER ALKYLIDENE-17A-LOWER ALKANOLYOXY-4-PREGNANE-3,20-DIONE WITH BORON TRIFLUORIDE IS A LOWER ALKANOL. PREFERRED COMPOUNDS ARE 6-METHOXY-16-LOWER ALKYLDENE-17A-LOWER ALKANOYLOXY-4,6-PREGNADIENE-3,20-DIONE WITH BORON TRIFLUORIDE IS A LOWER ALKANOL. PREFERRED COMPOUNDS ARE 6-METHOXY-16-LOWER ALKYLIDENE-17A-LOWER ALKANOYLOXY-4,6-PREGNADIENE-3,20-DIONES (PARTICULARLY 6-METHOXY-16-METHYLENE-17A-ACETOXY-4,6PREGNADIENE-3,20-DIONE) AND THEIR 1A,2A-CYCLOMETHYLENE DERIVATIVES, WHICH ARE VALUABLE IN THE TREATMENT OF BENIGN PROSTATIC HYPERTROPHY. THESE 6-METHOXY COMPOUNS ARE ALSO PREPARED BY REACTION OF A 16-LOWER ALKYLIDENE-17ALOWER ALKANOYLOXY-4-PREGNENE-3,20-DIONE OR A 3-ENOL ETHER OR 3-ENOL ESTER DERIVATIVE THEREOF WITH A CUPRIC HALIDE IN METHANOL. THE 1A,2A-CYCLOMETHYLENE-6-ALKOXY-16-LOWER ALKYLIDENE-17A-LOWER ALKANOYLOXY-4,6-PREGNADIENE-3,20-DIONES ARE ALSO PREPARED FROM A 6-ALKOXY-16-LOWER ALKYLIDENE17A-LOWER ALKANOYLOXY-1,4,6-PREGNATRIENE-3,20-DIONE BY REACTION WITH DIMETHYLSULFOXONIUM METHYLIDE.
Inventors
- 👤 Richard Rausser
- 👤 Robert Tiberi
Bibliographic Details
Claims Analysis
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