Abstract

Both Aconitum hemsleyanum and Aconitum geniculatun have abundant contents of yunaconitine (1). Yunaconitine (1) has similar skeleton to crassicauline A (3); the only difference between them is that 1 contains a α-hydroxyl group at C-3. Our team attempts to convert 1 into 3 because 3 owns pharmacological activity. There are two steps to achieve the transformation above: firstly, use dehydration reaction to transform yunaconitine (1) into dehydroyunaconitine (2); secondly, use hydrogen reduction to acquire crassicauline A (3). Compared with other methods, this one below is more suitable for production application and more concise; moreover, the cost is lower with higher yield.

Graphic Abstract

中文翻译：

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从尤乌头碱部分合成粗茎碱 A。

摘要

Aconitum hemsleyanum和Aconitum geniculatun均含有丰富的云乌头碱(1)。尤乌头碱(1)与粗茎碱 A (3)具有相似的骨架；它们之间唯一的区别是1在C-3处含有α-羟基。我们团队试图将1转化为3，因为3具有药理活性。实现上述转化的步骤有两个：首先，利用脱水反应将云乌头碱(1)转化为脱氢云乌头碱(2)；其次，用氢还原得到粗茎碱A (3)。与其他方法相比，下面这个更适合生产应用，也更简洁；而且成本更低，产量更高。

图文摘要