【摘要】 <正> Stork和Ringold,报告了孕甾烯类化合物在四氢呋喃中用碘和氧化钙处理,可直接导入G₂₁-碘。此碘化物在无水丙酮中与醋酸钾反应,即成G₂₁-醋酸酯,两步反应的产率为60％。黄鸣龙等将此反应应用于可的松醋酸,酯的合成中,并在方法上稍加改进,两步反应的产率为59％。此后陆续见有将此法应用于甾体化合物的合成中,但产率往往欠佳。更多还原

【Abstract】 When we undertook the synthesis of Reichstein’s substance S acetate and cortisone acetate from 17 α-hydroxy-progesterone and 17 α-hydroxy-ll-oxo-progesterone respectively by Joly’s method, we introduced a modified procedure, in which chloroform and methyl alcohol were used as solvents in the synthesis of 21-iodo-intermediates, and the dimethylformamide as a solvent to convert 21-iodo-intermediate to 21-acetoxy steroids by reaction with anhydrous potassium acetate.After preliminary technical improvements, the yields of the synthesis of cortisone acetate and Reichstein’s substance S acetate from 17 α-hydroxy-ll-oxo-progesterone and 17 α-hydroxy-progesterone respectively were raised to a new level of 80.181.1％, which is higher than Joly’s method for about 10％ and higher than Ringold’s method for about 20％.更多还原