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一种经济有效的制备2,4,5-三氟苯乙酸的新方法

A Cost-effective New Method for Preparing 2,4,5-Trifluorophenylacetic Acid
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摘要 2,4,5-三氟苯乙酸是合成治疗Ⅱ型糖尿病药物的关键中间体,同时也是合成新型含氟除草剂的重要中间体。本文以2,3,5,6-四氟对苯二甲酸二乙酯为原料,通过亲核取代、水解和脱羧三步反应得到2,4,5-三氟苯乙酸,总产率达到92%以上。该合成方法工艺简单,产率高,适合工业化生产。 2,4,5-trifluorophenylacetic acid is a key intermediate in the synthesis of drugs for the treatment of type II diabetes mellitus,and is also an important intermediate in the synthesis of novel herbicides containing fluorine.In this paper,2,4,5-trifluorophenylacetic acid was obtained from diethyl 2,3,5,6-tetrafluoroterephthalatic acid by a three-step reaction of nucleophilic substitution,hydrolysis and decarboxylation.The total yield was more than 92%.The synthesis method is simple,high yield and suitable for industrial production.
作者 李秀珍 LI Xiu-zhen(Fujian Runhua Chemical Co.,Ltd.,Fujian 354003,China)
出处 《浙江化工》 CAS 2022年第2期9-11,共3页 Zhejiang Chemical Industry
关键词 2 3 5 6-四氟对苯二甲酸二乙酯 丙二酸二乙酯 氰乙酸乙酯 2 4 5-三氟苯乙酸 制备 diethyl 2,3,5,6-tetrafluoroterephthalatic acid diethyl malonate ethyl cyanoacetate 2,4,5 trifluorophenylacetic acid synthesis
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  • 1夏玲红.治疗糖尿病的新药西他列汀[J].中国新药杂志,2007,16(12):979-981. 被引量:26
  • 2FALCHI A, STIVANELLO M, SERAFINI S, et aI. Process for the Preparation of Fluorophenylacetic Acids and Derivatives Thereof[P]. WOz2008078350,2008-07-03.
  • 3THOMAS H O. Method for the Production of 2,4,5-Trimeth- ylphenylaeetie Aeid[P]. US: 2005182274,2005-08418.
  • 4ASTON J G,NEWKIRK J D,JENKINS D M,et al. Mandelic acid[J].Organic Syntheses, 1943,23,48-50.
  • 5HERMAN GA,BERGMAN A,STEVENS C,et al.Effect of single oral doses of sitagliptin,a dipeptidyl peptidase-4 inhibitor,on incretin and plasma glucose levels after an oral glucose tolerance test in patients with type 2 diabetes[J].J Clin Endocrinol Metab,2006,91 (11):4612-4619.
  • 6BERGMAN AJ,STEVENS C,ZHOU Y,et al.Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin,a dipeptidyl peptidase-Ⅳ inhibitor:a double-blind,randomized,placebo-controlled study in healthy male volunteers[J].Clin Ther,2006,28(1):55 -72.
  • 7HERMAN GA,BERGMAN A,LIU F,et al.Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitaglipin in middle-aged obese subjects[J].J Clin Pharmacol,2006,46(8):876 -886.
  • 8HERMAN GA,STEVENS C,VAN DYCK K,et al.Pharmacokinetics and pharmacodynamics of sitagliptin,an inhibitor of dipeptidyl peptidase Ⅳ,in healthy subjects:results from two randomized,double-blind,placebo-controlled studies with single oral doses[J].Clin Pharmacol Ther,2005,78(6):675 -688.
  • 9VINCENT SH,REED JR,BERGMAN AJ,et al.Metabolism and excretion of the DPP-4 inhibitor[14C] sitagliptin in humans[J].Drug Metab Dispos,2007,35(4):533 -538.
  • 10RAZ I,HANEFELD M,XU L,et al.Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitsgliptin as monotherapy in patients with type 2 diabetes mellitus[J].Diabetologia,2006,49(11):2564 -2571.

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