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。
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 acid of pleuromutilins, esterify with 2 - mercaptoacetic acid anhydride, hydrolysis and and aminate with 2 - （ removal 2 - hydroxyacetic 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%.
出处
《中国兽药杂志》
北大核心
2015年第8期45-50,共6页
Chinese Journal of Veterinary Drug
