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Process for Preparation of 3-g (a) -hydroxy, 3-g (b) -substituted Pregnants
Process for Preparation of 3-g (a) -hydroxy, 3-g (b) -substituted Pregnants
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机译:制备3-g(a)-羟基,3-g(b)-取代的孕妇的方法
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摘要
This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3 alpha -hydroxy,3 beta -substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereoselectively into a 3(R)-pregnan-3-spiro-2'oxirane-20-one intermediate. This intermediate can then be converted regioselectively by a second set of reactions to the 3 alpha -hydroxy,3 beta -substituted-20-one form, which can be further modified at the 20-keto position. Through this method, each ketone group is independently treated. By modifying the ketones one at a time, one can obtain the desired stereo-specificity at each site.
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