首页|16α-羟基泼尼松龙的合成工艺改进

16α-羟基泼尼松龙的合成工艺改进

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针对原 16α-羟基泼尼松龙合成工艺原料成本高、消除反应选择性差等问题,开发了一种改进工艺.以 21-羟基孕甾-1,4,9(11),16-四烯-3,20-二酮-21-醋酸酯为原料,经氧化、溴羟化、脱溴及水解等 4 步反应合成目标化合物 16α-羟基泼尼松龙,降低了生产成本及三废排放量,并使反应总收率达到 82.2%.产物结构经 1H NMR、13C NMR和MS(ESI)等数据确证.改进后的合成工艺具有反应选择性好、成本低、总收率高等优点.
Improvement for the Synthesis Process of 16α-Hydroxprednisolone
In view of the problem of high raw material cost and poor selectivity in elimination reaction of the original 16α-hydroxyprednisolone synthesis process,an improved process was developed.The target product 16α-hydroxyprednisolone was synthesized from 21-hydroxypregna-1,4,9(11),16-tetraene-3,20-dione-21-acetate by oxidation,hydroxybromination,debromination and hydrolysis.The production cost and waste emissions were reduced,and the total yield of the reaction reached 82.2%.The structure of product was confirmed by 1H NMR,13C NMR and MS(ESI).The improved synthetic process has the advantages of good selectivity,low cost and high total yield.

16α-hydroxprednisolone21-hydroxypregna-1,4,9(11),16-tetraene-3,20-dione-21-acetateoxidationhydroxybrominationprocess improvement

尹琳琳、王乐晓、陈益俊、金旦妮

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台州仙琚药业有限公司, 浙江 台州 317016

16α-羟基泼尼松龙 21-羟基孕甾-1,4,9(11),16-四烯-3,20-二酮-21-醋酸酯 氧化反应 溴羟化反应 工艺改进

2024

浙江化工
浙江省化工研究院有限公司

浙江化工

影响因子:0.131
ISSN:1006-4184
年,卷(期):2024.55(1)
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