CAS: 220141-74-2; 2,4,5-Trifluorobenzyl Cyanide

上下游产品

sodium cyanide 1-(chloromethyl)-2,4,5-trifluorobenzene 1,2,4-trifluorobenzene 2,4,5-Trifluoro-toluene 4-cyano-4-(2,4,5-trifluorophenyl)heptanedioic acid dimethyl ester 1-(2,4,5-trifluorophenyl)pent-4-en-2-amine (S)-1-(2,4,5-trifluorophenyl)pent-4-en-2-amine 5-cyano-2-oxo-5-(2,4,5-trifluorophenyl)cyclohexanecarboxylic acid methyl ester

4,5-二氯-2-硝基甲苯置于盐酸,Potassium Fluoride,Tetrafluoroboric Acid,偶氮二异丁腈,四丁基溴化铵,氢气,Sodium Nitrite体系中,用 环丁砜,甲醇,水,二甲基亚砜 用作溶剂,-40.0~180.0 °C,8.0 Mpa 条件下,反应 15.0H,反应生成2,4,5-三氟苯乙腈
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-11174266-B2
优先权日:2018-02-13
标 题 :Efficient process for the preparation of sitagliptin
发明人：SHI TERRY; LOU SAM; DE LUCCHI OTTORINO; PADOVAN PIERLUIGI
权利人:F I S —FABBRICA ITALIANA SINTETICI S P A
摘要:Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.

专利号:CN-117466729-A
优先权日:2023-12-28
标题:A kind of synthesis method of 2,4,5-trifluorophenylacetic acid

专利号:CN-118598879-A
优先权日:2024-06-26
标题:Synthesis method of sitagliptin intermediate