|
|
|
| Study on the synthesis process of epalrestat |
| Yang Cangjun |
| Hebei Jiheng Pharmaceutical Corporation Ltd., Hengshui 053400, China |
|
|
|
|
Abstract A synthetic method for the active pharmaceutical ingredient iprastam, which uses glycine as the starting material and undergoes addition, substitution, and cyclization reactions to obtain the intermediate I3-carboxymethyl rhodanine were provided. Intermediate II was obtained through condensation reaction using benzaldehyde and propanal as raw materials α- Methylcinnamaldehyde. Intermediate I and intermediate II undergo a condensation reaction to obtain crude iparameta and refined into finished products. The total yield of the product in the entire process is over 60%, with a purity of up to 99.24%, which meets the relevant quality standards. This synthesis process has a simple route, convenient operation, simple post-treatment, and is suitable for industrial production.
|
|
|
|
|
|
| [ 1 ] 黄祖斌,陈忠平. 依帕司他联合硫辛酸治疗老年糖尿病周围神经病变的临床效果[ J ]. 糖尿病新世界,2023,26( 13 ): 165 - 168.
[ 2 ] 孙 菲. 加巴喷丁联合依帕司他治疗糖尿病痛性神经病变的疗效[ J ]. 中国现代药物应用,2022,16( 12 ): 123 - 125.
[ 3 ] 程铁毛. 依帕司他对糖尿病肾病的治疗作用研究[ J ]. 实用糖尿病杂志,2020,16( 1 ): 55 - 56.
[ 4 ] 邬 磊,刘鹏鹰. 依帕司他治疗糖尿病周围神经病变大鼠的疗效评价[ J ]. 实用临床医药杂志,2013,17( 13 ):4 - 7.
[ 5 ] 陈华生,李海波,冼朝丽,等. 依帕司他联合和血明目片与羟苯磺酸钙对改善糖尿病视网膜病变的效果分析[ J ]. 世界复合医学,2023,9( 7 ): 185 - 187,191.
[ 6 ] 颜世强,郭 伟,何淑旺,等. 依帕司他合成工艺优化[ J ]. 食品与药品,2022,24( 3 ): 215 - 217.
[ 7 ] 刘向红,杨亚军,李兆林,等. 高纯度依帕司他的制备方法[ J ]. 石油化工应用,2018,37( 11 ): 115 - 119.
[ 8 ] 李月珍,赖宜生,梁臣艳. 依帕司他的合成工艺研究[ J ]. 中国药物化学杂志,2001( 3 ): 43 - 45.
[ 9 ] 冯建鹏,祝传宝,张虎跃,等. 高纯度依帕司他的制备方法[ J ]. 广东化工,2012,39( 11 ): 41 - 42.
[ 10 ] 刘向红,杨亚军,李兆林. 高纯度依帕司他的制备方法[ J ]. 石油化工应用,2018( 11 ):159 - 163.
[ 11 ] 吴弘辰,李琪荣,武亚明. 一种高纯度3α-羟基-7-氧代-5β-胆烷酸的制备方法[ J ]. 苏盐科技,2018( 1 ):16 - 19.
[ 12 ] 吴弘辰,李琪荣,武亚明. 一种高纯度3α-羟基-7-氧代-5β-胆烷酸的制备方法[J].现代盐化工,2018( 1 ):33 - 36.
[ 13 ] 匡青芬,陈新朋,杨笃才. 高纯度凝血因子Ⅸ制剂的制备方法[ J ]. 临床医药实践,2016( 6 ):25 - 26.
[ 14 ] 张治华. 低聚磷酸酯的高纯度高收率制备方法[ C ]. 中国塑料加工工业协会2009年塑料助剂生产与应用技术信息交流会,2009.
[ 15 ] 马清华,栾丽丽,曾丽娟,等. 桂芎通脉足浴方联合依帕司他治疗2型糖尿病周围神经病变的疗效观察[ J ]. 实用中西医结合临床,2022( 9 ):15 - 19.
[ 16 ] 韩 敏. 依帕司他辅助治疗糖尿病周围神经病变的效果探讨[ J ]. 名医,2022( 11 ):36 - 39.
[ 17 ] 廖志强. 探讨依帕司他治疗糖尿病周围神经病变的临床研究[ J ]. 糖尿病新世界,2020( 7 ):47 - 48.
[ 18 ] 张 伟. 依帕司他治疗糖尿病周围神经病变疗效观察[ J ]. 临床医药文献电子杂志,2019( 49 ):32 - 35.
[ 19 ] 朱丽晔. 依帕司他治疗糖尿病周围神经病变的效果观察[ J ]. 当代医学,2018( 28 ):14 - 16.
[ 20 ] 魏 东. 依帕司他片治疗糖尿病并发周围神经病变的临床效果研究[ J ]. 中国处方药,2016( 4 ):49 - 53.
[ 21 ] 熊伟华. 依帕司他联合α-硫辛酸治疗糖尿病周围神经病变[ J ]. 中国实用医药,2021( 8 ):58 - 61. |
|
|
|