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Position: Home > Articles > Improvement of Synthesis Technology of Tiamulin Fumarate Chinese Journal of Veterinary Drug 2015,49 (8) 45-50

延胡索酸泰妙菌素合成工艺改进

作  者:
赵伯龙;冶建军;张萍;李晓楠
单  位:
宁夏泰瑞制药股份有限公司
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
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。
译  名:
Improvement of Synthesis Technology of Tiamulin Fumarate
作  者:
ZHAO Bo-Long;YE Jian-jun;ZHANG Ping;LI Xiao-nan;Ningxia Taitui Pharmactlal Co.,Ltd;
关键词:
pleuromulin;;tiamulin fumarate;;2-(diethylamino)ethanethiol;;2-(diethylamino)ethanol
摘  要:
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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