CAS: 10184-69-7; Pregna-1,4,9(11)-Triene-17α,21-Diol-3,20-Dione

上下游产品

anecortaveprednisolon prednisolone 21-acetate

📜四烯孕二酮置于过氧化乙酸叔丁酯,氢溴酸,苄基三甲基氢氧化铵,对甲苯磺酸,Sodium Hydroxide体系中,用 四氢呋喃,二氯甲烷,丙酮 用作溶剂,化学反应 11.5H,反应生成泼尼松杂质d
参考文献:一种从甾醇发酵物合成二氟泼尼酯的方法
标题:一种从甾醇发酵物合成二氟泼尼酯的方法
摘要:本发明提供了一种从甾醇发酵物合成二氟泼尼酯的方法.以油脂工业副产品中含量极为丰富的植物甾醇发酵而来的甾醇发酵物9α-羟基-雄甾-1,4-二烯-3,17-二酮(9α-Oh-Ad)为起始原料,经历甾体9位羟基脱水成双键,17位羰基加乙炔,脱水,酸性下生成21位酮羰基,16,17位双键环氧化,高碘化物氧化引入21位羟基,16,17位α环氧氢溴酸开环,16β溴氢化脱除,成环原酸酯,开环,酯基化,9,11双键β环氧化,烯醇化酯化,6位亲电氟代和9,11环氧氟代开环,共15步反应.利用高碘化物氧化及环氧开环,脱溴高效构建了甾体17α,21-二羟基,得到重要中间体式11化合物,整个过程有效避免了传统工业生产皮质激素类药物所产生的大量重金属污染物铬,绿色环保适合工业化生产.

专利信息

专利号:US-4404141-A
优先权日:1981-03-09
标 题:Δ9(11) - And Δ16 -21-chloro-20-keto steroids of the pregnane and D-homopregnane series, their preparation and use as intermediates for the synthesis of highly effective corticoids
发明人：ANNEN KLAUS; LAURENT HENRY; HOFMEISTER HELMUT
权利人:SCHERING AG
摘要:Δ 16 - and Δ 17 -21-chloro-20-keto steroids of the formula ##STR1## wherein n is 1 or 2, n C 1 C 2 and C 9 C 11 represent a CC-single or CC-double bond, n R 1 is H or OH, n R 2 is H or CH 3 , n R 3 is H or F wherein, when R 3 =F, C 9 C 11 is a CC-single bond, and n R 4 is H, CH 3 , or F, n are valuable intermediates for preparation of highly effective, known steroids. n A process for preparing these compounds involves heating the corresponding 11β- and/or 17α- or 17aα-nitrooxy-21-mesyloxy-20-keto steroids with lithium chloride in a dipolar aprotic solvent at temperatures above room temperature.

专利号:EP-0061416-A1
优先权日:1981-03-09
标题 :Process for the preparation of Delta 9(11)- and delta 16-21-chloro-20-keto steroids of the pregnane and D-homopregnane series and their use as intermediates for the synthesis of highly effective corticoids