CAS: 887267-34-7; 1,2,4-Trifluoro-5-Methylbenzene

上下游产品

1,2-dichloro-4-methyl-5-nitrobenzene 1,2-difluoro-4-methyl-5-nitrobenzene 4,5-difluoro-2-methylaniline

4,5-二氯-2-硝基甲苯置于potassium Fluoride,Tetrafluoroboric Acid,四丁基溴化铵,氢气,Sodium Nitrite体系中,用 环丁砜,甲醇,水 作为反应溶剂,-40.0~180.0 °C,8.0 Mpa 条件下,反应 7.0H,反应生成 2,4,5-三氟甲苯
参考文献:一种2,4,5-三氟苯乙酸的制备方法
标题:一种2,4,5-三氟苯乙酸的制备方法
摘要:本申请属于药物中间体制备技术领域,公开一种2,4,5‑三氟苯乙酸的制备方法,包括:步骤一,将原料,季铵盐催化剂,环丁砜,氟化钾,反应得第一中间体;步骤二,第一中间体加氢催化反应得第二中间体;步骤三,第二中间体与氟化试剂成盐反应,骤冷,再与亚硝酸钠水溶液重氮化反应,得重氮盐;步骤四,重氮盐经高温裂解,得2,4,5‑三氟甲苯;步骤五至七,将2,4,5‑三氟甲苯依此经卤代,氰化,水解反应,得2,4,5‑三氟苯乙酸.本申请采用的原料易得且成本较低,每一步获得的对应产物的收率均较高,利于2,4,5‑三氟苯乙酸的大生产化.

专利信息

专利号:US-6870067-B2
优先权日:2002-10-08
标 题 :Process for the synthesis of trifluorophenylacetic acids
发明人：IKEMOTO NORIHIRO; DREHER SPENCER D
权利人:MERCK & CO INC
摘要:The present invention is concerned with a process for the preparation of trifluorophenylacetic acids using a Grignard reagent and an allylating agent, such as allyl bromide.

专利号:WO-2013114173-A1
优先权日:2012-01-30
标题:A novel process for the preparation of sitagliptin
发明人：MALLELA SAMBHU PRASAD SARMA; HAVALE SHRIKANT HANUMANTAPPA; BODDEPALLI NAGABHUSHANA RAO; GUNJI NAGARJUNA; MOKKAPATI BHAVANI SANKAR
权利人:SMILAX LAB LTD; MALLELA SAMBHU PRASAD SARMA; HAVALE SHRIKANT HANUMANTAPPA; BODDEPALLI NAGABHUSHANA RAO; GUNJI NAGARJUNA; MOKKAPATI BHAVANI SANKAR
摘要:The present invention is directed to a process for the preparation of enantiomerically enriched β-amino acid derivatives which are important chiral building blocks and intermediates in pharmaceuticals. More specifically, the invention pertains to a novel process for practically convenient and economically producing enantiomerically enriched β-amino acid derivatives which are useful for the synthesis of amide inhibitors of dipeptidyl peptidase IV like Sitagliptin, which have been used to treat type 2 diabetes.

专利号:US-8455479-B2
优先权日:2008-01-24
标 题 :Heterocyclic compounds
发明人：JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; SINGH NISHAN; NANDA GURMEET KAUR; MAGADI SITARAM KUMAR; SHARMA SUDHIR KUMAR
权利人:JAIN RAJESH; TREHAN SANJAY; DAS JAGATTARAN; SINGH NISHAN; NANDA GURMEET KAUR; MAGADI SITARAM KUMAR; SHARMA SUDHIR KUMAR; PANACEA BIOTEC LTD
摘要:The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more conditions that may be regulated or normalized via inhibition of dipeptidyl peptidase IV (DPP-IV).

专利号:US-2007276139-A1
优先权日:2004-02-10
标题:Substituted Pixyl Protecting Groups for Oligonucleotide Synthesis
发明人：SONG QUANLAI; KHAMMUNGKHUNE SAK; ROSS BRUCE S; GRIFFEY RICHARD H
权利人:SONG QUANLAI; KHAMMUNGKHUNE SAK; ROSS BRUCE S; GRIFFEY RICHARD H
摘要:The present invention describes an improved hydroxyl protecting group of formula (1), wherein R 2 and R 7 are specified substituents and Q is O, S, NR 10 or N(Câ•?O)R 10 .

专利号:CN-102574856-B
优先权日:2009-05-11
标 题:The synthesis of sitagliptin

专利号:US-2004077901-A1
优先权日:2002-10-08
标题:Process for the synthesis of trifluorophenylacetic acids