Verfahren zur Herstellung von 4-Hydroxy-19-nortestosteron-17-cyclopentyl-propionat

The invention comprises 4-hydroxy-19-nortestosterone 17-b - cyclopentylpropionate and the preparation thereof by treating 4,5-epoxy-19-nortestosterone 17-b -cyclopentylpropionate with sulphuric acid in an organic solvent, e.g. acetic acid. The above process may be modified in that the 4,5-epoxy-19-nortestosterone 17-b -cyclopentylpropionate is prepared by acylating 4,5-epoxy-19-nortestosterone with a b -cyclopentylpropionic acid halide such as the chloride, in the presence of a tertiary amine, and the 4,5-epoxy-19-nortestosterone may be prepared by treating 19-nortestosterone with hydrogen peroxide in an alkaline medium. Detailed examples are given.ALSO:A therapeutic composition comprises 4-hydroxy - 19 - nortestosterone 17 - b - cyclopentylpropionate and compatible pharmaceutically acceptable carrier. The composition may be in the form of a solution in a fluid vehicle in the form of a gel or in the form of a microcrystalline suspension in an aqueous medium.