| 摘要 |
<p>The invention comprises the 16a -propanolid and the 17a -propanolid of, respectively, 16b -hydroxy - androst - 4 - en - 3 - one and 17b -hydroxy - androst - 4 - en - 3 - one, and a process for preparing 16- or 17-propanolids of unsaturated steroids from a 16- or 17-keto steroid by protecting other groups if necessary, followed by condensation with a Grignard magnesium derivative of a 5 - (b - haloethyl)-2,2-dialkyl-1,3-dioxolane to form the corresponding 16b - hydroxy - 16a - or 17b -hydroxy-17a - (11,21 - dihydroxy - 4 - butyl) steroid in the form of its 11,21-ketonide, liberating the protecting group or groups, treating the product with an oxidizing agent to effect simultaneous degradation and cyclization of the side-chain to form the corresponding 11,16b -epoxy-16a - or 11,17b - epoxy - 17a - (11#x - hydroxypropyl) derivative, and oxidizing this simultaneously or consecutively to form the desired lactone. The compounds of the invention have aldosteronic activity.</p> |
