贝诺酯合成工艺综述与对比分析
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摘要
贝诺酯是阿司匹林和扑热息痛的酯化产物,是一种效果优良的非甾体类解热、镇痛、抗炎药,临床应用广泛.在贝诺酯的合成工艺路线以及致力于经济、环保且高收率的工艺优化报道的基础上,通过大量查阅分析,对贝诺酯的合成工艺进行综述,对常用工艺路线的优化策略进行总结,并对各种不同合成方法的优缺点进行了对比分析,为贝诺酯的相关研究提供参考并为开展孪药合成研究奠定理论基础.
Benorilate is the esterification product of aspirin and paracetamol. It is an effective anti-inflammatory,antipyretic and analgesic drug of non steroids,and has been widely used in clinical practice. There are not manyreports on the synthetic process of benorilate,and many reports are devoted to economic,environmental protectionand high yield process optimization. In this paper,a large number of literatures have been investigated,thesynthesis technology of Benorilate has been reviewed,the optimization strategies of common process routeshave been summarized,and the advantages and disadvantages of various synthesis methods have been comparedand analyzed,which provides reference for the study of Benorilate and lays a theoretical foundation for the author'songoing research on the synthesis of twin drugs.
Benorilate is the esterification product of aspirin and paracetamol. It is an effective anti-inflammatory,antipyretic and analgesic drug of non steroids,and has been widely used in clinical practice. There are not manyreports on the synthetic process of benorilate,and many reports are devoted to economic,environmental protectionand high yield process optimization. In this paper,a large number of literatures have been investigated,thesynthesis technology of Benorilate has been reviewed,the optimization strategies of common process routeshave been summarized,and the advantages and disadvantages of various synthesis methods have been comparedand analyzed,which provides reference for the study of Benorilate and lays a theoretical foundation for the author'songoing research on the synthesis of twin drugs.
引文
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[2] Sterwin. p-Aminophenyl salicylates:NL 654517[P]. 1965-07-24.
[3] Portelli. Process for the preparation of benorilate:CA 1035782[P]. 1973-08-13.
[4] SALAT F. Salicylic acid derivative:ES 457185[P]. 1978-08-04.
[5]李霞辉,张伟,龚永平,等. 4-二甲氨基吡啶催化合成贝诺酯[J].四川农业大学学报,2016,34(1):110-114.
[6]滕小波,钱捷.贝诺酯的合成进展[J].山东化工,2009,38(8):23-25.
[7]韩长日.扑炎痛的合成新法[J].精细石油化工,1994(1):45-46.
[8]王远亮,王建华.一类药用乙酰水杨酸酯衍生物的光气法合成新工艺:CN 1337391A[P]. 2001-08-17.
[9]熊琳.固体光气法合成乙酰水杨酰基硫脲衍生物和贝诺酯[D].兰州:西北师范大学,2010:52-62.
[10]傅晓钟,李零,饶光玲,等.贝诺酯合成工艺的改进[J].贵阳医学院学报,2012,37(4):440-443.
[11]姜志猛,蒋平,王卉.扑炎痛合成工艺的改进[J].医药工业,1985,16(11):28-29.
[12]刘娇,刘佳,张银羽,等.贝诺酯合成实验反应条件的优化[J].湖南学院学报,2016,37(5):18-21.
[13]王莹.贝诺酯的合成及表征[J].实验科学与技术,2014,12(4):32-34.
[14] ROBERTSON A. Amino-phenol compounds:US 3431293[P]. 1969-03-04.
[15] MONDELO C. 4-Acetamidophenyl-2-(acetyloxy)benzoate:ES 444802[P]. 1977-01-13.
[16]张明玉,张培兴.水杨酸衍生物-贝诺酯的合成[J].中国药学杂志,1989(9):544-545.
[17]唐维高,彭崇莹,邓元伟.扑炎痛合成工艺:CN1067881A[P]. 1991-06-17.
[18]艾庆霞.贝诺酯合成工艺的改进[J].中国医药工业杂志,1995,26(12):532-533.
[19]李晓媛.扑炎痛的合成研究[J].化工管理,2014(14):122.
[20]吴夏茂,肖柑媛,尹红梅,等.合成贝诺酯实验的优化与实践[J].实验科学与技术,2014,12(6):21-24.
[21]郑时龙,何凌,麦妙,等.贝诺酯的相转移催化合成[J].中国现代应用药学,1997,14(5):29-30.
[22]刘宝,李晓新,王玮.贝诺酯的相转移催化合成[J].开封医专学报,2000,19(1):37.
[23]王文静,吕玮,卢泽.贝诺酯的合成[J].河南大学学报(医学版),2006,25(1):39-42.
[24]韩立伟,白术杰.贝诺酯合成的工艺改进[J].黑龙江医药科学,2007,30(2):26.
[25]沈广志,邹桂华,才玉婷.消炎镇痛药贝诺酯的合成[J].辽宁化工,2009,38(2):94-95.
[26]张丽.解热镇痛药贝诺酯的合成工艺优化[J].才智,2011(35):357.
[27]翟媛媛.解热镇痛药贝诺酯的合成[J].化工管理,2016(20):60.
[28]王瑾,孙微.贝诺酯的原料制备及其表征[J].化学与黏合,2009,31(6):33-35.
[29]李婉茹,王树辉.贝诺酯合成工艺的改进[J].黑龙江医药科学,2000,23(4):53-54.
[30]陈旭冰,陈光勇,施贵荣,等.贝诺酯的合成工艺改进[J].大理学院学报,2009,8(6):12-14.
[31]戴国兴,王磊,陈守涛.贝诺酯催化合成工艺的研究[J].煤炭与化工,2014,37(8):79-81.
[32]马艳.扑炎痛合成工艺优化[J].化工时刊,2014,28(3):19-20.
[33]程先超,符敬伟,周慧,等.药物化学实验教学中异法同步模式的探索[J].实验室科学,2016,19(2):31-34.
[34]范兴山,王飞龙,吴双俊,等. 4-二甲氨基吡啶催化酯化合成贝诺酯的方法:CN 101844997B[P]. 2012-12-19.
[2] Sterwin. p-Aminophenyl salicylates:NL 654517[P]. 1965-07-24.
[3] Portelli. Process for the preparation of benorilate:CA 1035782[P]. 1973-08-13.
[4] SALAT F. Salicylic acid derivative:ES 457185[P]. 1978-08-04.
[5]李霞辉,张伟,龚永平,等. 4-二甲氨基吡啶催化合成贝诺酯[J].四川农业大学学报,2016,34(1):110-114.
[6]滕小波,钱捷.贝诺酯的合成进展[J].山东化工,2009,38(8):23-25.
[7]韩长日.扑炎痛的合成新法[J].精细石油化工,1994(1):45-46.
[8]王远亮,王建华.一类药用乙酰水杨酸酯衍生物的光气法合成新工艺:CN 1337391A[P]. 2001-08-17.
[9]熊琳.固体光气法合成乙酰水杨酰基硫脲衍生物和贝诺酯[D].兰州:西北师范大学,2010:52-62.
[10]傅晓钟,李零,饶光玲,等.贝诺酯合成工艺的改进[J].贵阳医学院学报,2012,37(4):440-443.
[11]姜志猛,蒋平,王卉.扑炎痛合成工艺的改进[J].医药工业,1985,16(11):28-29.
[12]刘娇,刘佳,张银羽,等.贝诺酯合成实验反应条件的优化[J].湖南学院学报,2016,37(5):18-21.
[13]王莹.贝诺酯的合成及表征[J].实验科学与技术,2014,12(4):32-34.
[14] ROBERTSON A. Amino-phenol compounds:US 3431293[P]. 1969-03-04.
[15] MONDELO C. 4-Acetamidophenyl-2-(acetyloxy)benzoate:ES 444802[P]. 1977-01-13.
[16]张明玉,张培兴.水杨酸衍生物-贝诺酯的合成[J].中国药学杂志,1989(9):544-545.
[17]唐维高,彭崇莹,邓元伟.扑炎痛合成工艺:CN1067881A[P]. 1991-06-17.
[18]艾庆霞.贝诺酯合成工艺的改进[J].中国医药工业杂志,1995,26(12):532-533.
[19]李晓媛.扑炎痛的合成研究[J].化工管理,2014(14):122.
[20]吴夏茂,肖柑媛,尹红梅,等.合成贝诺酯实验的优化与实践[J].实验科学与技术,2014,12(6):21-24.
[21]郑时龙,何凌,麦妙,等.贝诺酯的相转移催化合成[J].中国现代应用药学,1997,14(5):29-30.
[22]刘宝,李晓新,王玮.贝诺酯的相转移催化合成[J].开封医专学报,2000,19(1):37.
[23]王文静,吕玮,卢泽.贝诺酯的合成[J].河南大学学报(医学版),2006,25(1):39-42.
[24]韩立伟,白术杰.贝诺酯合成的工艺改进[J].黑龙江医药科学,2007,30(2):26.
[25]沈广志,邹桂华,才玉婷.消炎镇痛药贝诺酯的合成[J].辽宁化工,2009,38(2):94-95.
[26]张丽.解热镇痛药贝诺酯的合成工艺优化[J].才智,2011(35):357.
[27]翟媛媛.解热镇痛药贝诺酯的合成[J].化工管理,2016(20):60.
[28]王瑾,孙微.贝诺酯的原料制备及其表征[J].化学与黏合,2009,31(6):33-35.
[29]李婉茹,王树辉.贝诺酯合成工艺的改进[J].黑龙江医药科学,2000,23(4):53-54.
[30]陈旭冰,陈光勇,施贵荣,等.贝诺酯的合成工艺改进[J].大理学院学报,2009,8(6):12-14.
[31]戴国兴,王磊,陈守涛.贝诺酯催化合成工艺的研究[J].煤炭与化工,2014,37(8):79-81.
[32]马艳.扑炎痛合成工艺优化[J].化工时刊,2014,28(3):19-20.
[33]程先超,符敬伟,周慧,等.药物化学实验教学中异法同步模式的探索[J].实验室科学,2016,19(2):31-34.
[34]范兴山,王飞龙,吴双俊,等. 4-二甲氨基吡啶催化酯化合成贝诺酯的方法:CN 101844997B[P]. 2012-12-19.