具有16-α-甲基甾体类药物中间体的制备方法

Method for preparing steroid drug intermediate with 16-alpha-methyl

Abstract

The invention provides a method for preparing a steroid drug intermediate with 16-alpha-methyl. In the method, a steroid compound I is selected as an initiator to take part in Grignard reaction to transform the sixteenth bit thereof so as to obtain a Grignard product; the Grignard product takes part in epoxy reaction to transform the seventeenth bit thereof to obtain a Grignard epoxy product; and the Grignard epoxy product takes part in hydrolysis reaction to transform the third bit thereof and perform open loop on the seventeenth bit and the twentieth bit thereof to obtain a steroid compound II which is the steroid drug intermediate with 16-alpha-methyl. The steroid compound II with 16-alpha-methyl is usually used for preparing common clinical meqoeofrol acefate, such as dexamethasone, dexamethasone sodium phosphate, mometasone furoate, dexamethasone acetate and the like.
本发明提供了一种具有16-α-甲基甾体类药物中间体的制备方法,选择甾体化合物I为起始物进行经格氏反应对16位改造得到格式产物,然后用格式产物进行环氧反应对17位改造得到格式环氧产物,最后用格式环氧产物进行水解反应对3位改造和对17、20位开环,得到具有16-α-甲基甾体类药物中间体甾体化合物II,该具有16-α-甲基的甾体化合物II常用于制备临床上常用的糖皮质激素类药物,例如:地塞米松,地塞米松磷酸钠,糠酸莫米他松,地塞米松醋酸酯等。

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    《Organic Process Research & Development》 19971231 Tetsuo Ohta等 "Improved Synthetic Route to Dexamethasone Acetate from Tigogenin " 421页第2栏实验部分-422页第1栏、图表2 1-9 第1卷, 第6期 2

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    CN-105399791-AMarch 16, 2016江苏远大仙乐药业有限公司一种倍他米松中间体的制备方法