广州化工
廣州化工
엄주화공
GUANGZHOU CHEMICAL INDUSTRY AND TECHNOLOGY
2012年
7期
112-113,122
,共3页
西酞普兰%酰化%闭环%工业化生产
西酞普蘭%酰化%閉環%工業化生產
서태보란%선화%폐배%공업화생산
citalopram%acylation%closed loop%industrial production
西酞普兰是一种已经上市多年的抗抑郁症药物,具有巨大的市场价值。本文在专利US4943590报道的工艺基础上进行改进,以4-[4-（二甲胺基）-1-（4-氟苯基）-羟基丁基]-3-（羟甲基）-苯腈为起始原料,以甲苯为溶剂,以对甲苯磺酰氯为酰化试剂,以20%的碳酸钠水溶液为缚酸剂,于0℃反应制备西酞普兰。产品经提纯后,其纯度可达到99.5%以上。该工艺的转化率在99%以上,具有工艺操作条件温和,原料价廉易得,三废排放少的优点,完全可以满足工业化生产的要求。
西酞普蘭是一種已經上市多年的抗抑鬱癥藥物,具有巨大的市場價值。本文在專利US4943590報道的工藝基礎上進行改進,以4-[4-（二甲胺基）-1-（4-氟苯基）-羥基丁基]-3-（羥甲基）-苯腈為起始原料,以甲苯為溶劑,以對甲苯磺酰氯為酰化試劑,以20%的碳痠鈉水溶液為縳痠劑,于0℃反應製備西酞普蘭。產品經提純後,其純度可達到99.5%以上。該工藝的轉化率在99%以上,具有工藝操作條件溫和,原料價廉易得,三廢排放少的優點,完全可以滿足工業化生產的要求。
서태보란시일충이경상시다년적항억욱증약물,구유거대적시장개치。본문재전리US4943590보도적공예기출상진행개진,이4-[4-（이갑알기）-1-（4-불분기）-간기정기]-3-（간갑기）-분정위기시원료,이갑분위용제,이대갑분광선록위선화시제,이20%적탄산납수용액위박산제,우0℃반응제비서태보란。산품경제순후,기순도가체도99.5%이상。해공예적전화솔재99%이상,구유공예조작조건온화,원료개렴역득,삼폐배방소적우점,완전가이만족공업화생산적요구。
Citalopram was an effective and safe antidepressant which existed in the market for many years and had great market value.To realize the industrial production of citalopram,the process was improved based on the patent US4943590.The improved process was 4-（4-（dimethylamino）-1-（4-fluorophenyl）-hydroxy-butyl）-3-（hydroxymetheyl）-benzonitrile was dissolved in toluene at 0 ℃.Toluene sulfochloride was used as acylation reagent,HCl generated in the acylation reaction was absorbed by Na2CO3 water solution（20 wt-%）.The conversion rate of the process was higher than 99%,and the purity of the product was more than 99.5%.This improved process was very easy to carry out,those chemical materials were commercialized and cheep,and low pollutant discharge,which can satisty the need of industrialized production.
