Process for the preparation of 17 alpha -bromoethynyl- and 17 alpha -iodoethynyl-17 beta -hydroxy steroids and novel products thereof

摘要

A process for preparing bromine- or iodine-unlabeled or radioactively labeled 17 alpha -bromoethynyl- and 17 alpha -iodoethynyl-17 beta -hydroxy steroids of the androstane and estrane series of the partial formula <IMAGE> wherein is a single bond or a double bond, V is a carbon-carbon bond or a methylene group, R is hydrogen or methyl, and X is bromine or iodine, from corresponding 17 alpha -ethynyl-17 beta -hydroxy steroids, comprises treating the starting steroid in an inert solvent with a brominating agent or an iodinating agent in the presence of a silver salt. The process enables production of old and new compounds having value as pharmacologically active compounds and also as diagnostic agents when the iodine or bromine is radioactive.