| 摘要: |
| 以精制的截短侧耳素为原料，经对甲苯磺酰氯磺化后，与二甲基半胱胺盐酸盐反应，制得截短侧耳素半胱胺取代物；另外由D-缬氨酸、乙酰乙酸甲酯和氢氧化钾反应制得（R）-2-（1-甲氧羰基-2-烯丙基）氨基-3-甲基丁酸钾，经氯甲酸乙酯活化后与截短侧耳素半胱胺取代物反应，最后通过调节pH值，经反相萃取后，冻干得盐酸沃尼妙林，总收率为69%，所得产品按照EP6.0进行了质量检测，产品具有含量高、杂质少等优点。 |
| 关键词: 盐酸沃尼妙林 合成 截短侧耳素 |
| DOI： |
| 投稿时间：2014-07-14修订日期：2014-09-11 |
| 基金项目: |
|
| The Synthesis of New Veterinary Drug Valnemulin hydrochloride |
|
| (Wuhan Hvsen Biotechnology Co., Ltd., Hubei Province Veterinary Drug Engineering Research Center) |
| Abstract: |
| Pleuromutilin refined as raw material and reacted with the sulfonated toluene sulfonyl chloride, dimethyl cysteamine hydrochloride to prepare cysteamine substituent; D-valine and methyl acetoacetate were reacted with potassium to obtain (R)-2-(1-methoxycarbonyl-2-allyl)amino-3-methylbut-potassium, follow by activated with ethyl chloroformate to react with pleuromutilin cysteamine substitution, and finally by adjusting the pH and inverting extraction to obtain valnemulin hydrochloride with the total yield of 69%. The product was tested according with EP6.0 to have high content and low impurities and so on. |
| Key words: hydrochloride Valnemulin synthesis study Pleuromutilin |
