| 摘要: |
| 使用乙酸酐对截短侧耳素11’-羟基进行保护，水解掉2-羟基乙酸，与2-巯基乙酸酯化，再与2-二乙氨基乙醇氨化，得到泰妙菌素。工艺中以2-二乙氨基乙醇代替2-二乙胺基乙硫醇作为侧链底物合成延胡索酸泰妙菌素，降低了有毒有害反应物对工业合成路线带来的额外成本。最终质量分数可达到920~960 mg/g。 |
| 关键词: 截短侧耳素 延胡索酸泰妙菌素 2-二乙胺基乙醇 2-巯基乙酸 |
| DOI： |
| 投稿时间：2015-06-03修订日期：2015-08-05 |
| 基金项目: |
|
| Improvement of Synthesis Technology of Tiamulin Fumarate |
|
| (Ningxia Taitui Pharmactlal Co.,Ltd) |
| Abstract: |
| Use 2-(diethylamino)ethanol instead of 2-(diethylamino)ethanethiol, as side-chain radical to synthesize tiamulin fumarate,In order to reduce the risk and the additional costs of that use the toxic chemicals. The protection against 11’ hydroxyl of pleuromutilins is acetic anhydride,hydrolysis and removal 2-hydroxyacetic acid of pleuromutilins,esterify with 2-mercaptoacetic acid and aminate with 2-(diethylamino)ethanol to Synthesis tiamulin fumarate. In the conclusion,the content of tiamulin fumarate is 920~960 mg/g,and the the yield of amount of substance is 87.7%.
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| Key words: pleuromulin tiamulin fumarate 2-(diethylamino)ethanethiol 2-(diethylamino)ethanol |
