| 摘要 |
<p>Tritiumllabelled steroids of formula (I) are new. (where T = tritium; Z = a blocked ketonic grp. which is a cyclic or non-cyclic ketal, thioketal, or mixed ketal, the cyclic bridges contg. 2-4C and the non-cyclic bridges contg. 1 or 2 C). (I) are prepd. by the following route: 3,17-beta - diacetoxy estra-1,3,5(10) 6-tetraene (II) is reduced by tritium in the presence of a catalyst, partic. palladium hydroxide to give 3, 17 beta-diacetoxy estra-1,3,5(10) triene 6,7-T2 (III). This is saponified with a strong base to give 3, 17 beta-dihydroxy-estra 1,3,5(10) triene 6,7-T2 (IV). The 3-OH grp. is alkylated, such as with dimethyl sulphate and the prod. undergoes a Birch reaction by the action of lithium in ammonia, to give 3-OR -17 beta hydroxyestra 2,5(10) diene 6,7-T2 (V) (where R = 1-4 C Alkyl) Treatment with weak acid gives 3-oxo 17 beta-hydroxy 5(10) estren 6,7-T2 (VI). This is treated with pyridinium perbromide to give 3-oxo-17 beta -hydroxy estra-4,9-diene 6,7-T2 (VII). This prod. is oxidised with aq. sulphochromic soln., and the 3-ketone gp. is ketalised.</p> |
