CAS: 209995-38-0; 2,4,5-Trifluorophenylacetic Acid

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CAS号1036273-14-9 2-(2,4,5-triflu... | CAS号680993-47-9 3-(2,4,5-triflu... | CAS号367-23-7 1,2,4-三氟苯 | CAS号868071-17-4 (3S)-2',4',5'-三... | CAS号764667-64-3 5-[1-羟基-2-(2,4,... | CAS号769195-26-8 3-氧代-4-(2,4,5-三... | CAS号764667-65-4 (2Z)-4-氧代-4-[3-... | CAS号654671-77-9 磷酸西他列汀 | CAS号486460-00-8 (3R)-N-叔丁氧羰基-3-... | CAS号1152439-73-0 2,2-Dimethyl-5-... | CAS号1169707-29-2 (2Z)-1-[5,6-Dih... | CAS号1204818-19-8 (R)-3-氨基-4-(2,4... | CAS号251366-49-1 α-bromo-(2,4,5-...

2,4-二氯氟苯置于potassium Fluoride,硫酸,硝酸,氯,Sodium Hydride,Sodium Hydroxide体系中,用 环丁砜,甲苯 用作溶剂,50.0~210.0 °C,101.33 Kpa 条件下,反应 29.0H,反应生成2,4,5-三氟苯乙酸
参考文献:2,4,5-三氟苯乙酸的制备方法
标题:2,4,5-三氟苯乙酸的制备方法
摘要:本发明公开了一种2,4,5‑三氟苯乙酸的制备方法,属于化学药物中间体制备方法技术领域,利用2,4‑二氯氟苯为原料,经硝化,氟化,氯代,偶联和水解反应制备2,4,5‑三氟苯乙酸.本发明方法,采用的原料相对廉价易得,工艺路线成熟,操作简单,收率较高,具有较高的工业化价值.

专利信息

专利号:US-11459549-B2
优先权日:2018-05-10
标 题:Method for biocatalytic synthesis of Sitagliptin and intermediate thereof
发明人：WU FAHAO; YANG WEN; LI GANG; SHI HONGWEI; GAO YANGZHE; LIU LILI; YUAN ZHIFA
权利人:CHINA FORTUNE WAY COMPANY; NANJING REDWOOD FINE CHEMICAL CO LTD
摘要:Provided is a method for biocatalytic synthesis of Sitagliptin and intermediates thereof, in particular, provided are compounds of Formula (I) and Formula (II), or pharmaceutically acceptable salts thereof, a polypeptide capable of catalyzing conversion of a compound of Formula (I) to a compound of Formula (II), a nucleic acid encoding the polypeptide, a vector and a cell comprising the nucleic acid. In addition, also provided are a method for producing a compound of Formula (II) and Sitagliptin by using the polypeptide and the compound of Formula (I), and a method for preparing the polypeptide.

专利号:US-8846916-B2
优先权日:2009-05-11
标题:Sitagliptin synthesis
发明人：GORE VINAYAK GOVIND; GADAKAR MAHESHKUMAR; BHOSLE PRIYANKA; SHINDE SURESH
权利人:GORE VINAYAK GOVIND; GADAKAR MAHESHKUMAR; BHOSLE PRIYANKA; SHINDE SURESH; GENERICS UK LTD
摘要:The present invention relates to novel processes for the preparation of enantiomerically enriched β-amino acid derivatives such as β-amino esters useful for the synthesis of enantiomerically enriched biologically active molecules such as sitagliptin. The key step involves the resolution of the racemate with mandelic acid.

专利号:US-10913747-B2
优先权日:2017-07-04
标题 :Efficient process for the preparation of sitagliptin through a very effective preparation of the intermediate 2,4,5-trifluorophenylacetic acid
发明人：DE LUCCHI OTTORINO; PADOVAN PIERLUIGI; BRASOLA ELENA
权利人:FIS FABBRICA ITALIANA SINTETICI SPA; 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:US-7468459-B2
优先权日:2003-03-19
标题:Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation
发明人：XIAO YI; ARMSTRONG III JOSEPH D; KRSKA SHANE W; NJOLITO EUGENIA; RIVERA NELO R; SUN YONGKUI; ROSNER THORSTEN
权利人:MERCK & CO INC
摘要:The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.

专利号:US-8765668-B2
优先权日:2010-06-04
标 题 :Methods of synthesis of β-aminobutyryl substituted compounds
发明人：STERK DAMJAN; USTAR MATJAZ; ZLICAR MARKO
权利人:STERK DAMJAN; USTAR MATJAZ; ZLICAR MARKO; LEK PHARMACEUTICALS
摘要:The present invention relates to process to prepare β-aminobutyryl compounds having β-amino acid core structural moieties and optionally having γ-phenyl and/or heterocyclic structural moieties. Such compounds are useful as key structure framework of modern drug chemistry.

专利号:US-8476437-B2
优先权日:2008-08-27
标题:Process for preparation of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine and new impurities in preparation thereof
发明人：KOTHARI HIMANSHU MADHUSUDAN; DAVE MAYANK GHANSHYAMBHAI; PANDEY BIPIN; SHUKLA BHAVIN SHRIPRASAD
权利人:KOTHARI HIMANSHU MADHUSUDAN; DAVE MAYANK GHANSHYAMBHAI; PANDEY BIPIN; SHUKLA BHAVIN SHRIPRASAD; CADILA HEALTHCARE LTD
摘要:The present invention relates to synthesis of β-amino acid derivatives of formula (I) and its salts of formula (Ia) by a novel process. The process comprises the reduction of a protected or unprotected prochiral β-amino acrylic acid or derivative there of, by using borane containing reducing agents at atmospheric pressure. The resulting racemic β-amino compound is resolved to a pure stereoisomer of formula (I), specifically to (2R)-4-oxo-4-[3-Ctrifluoromethyl)-5,6-dihydrol[1,2,4]triazolo[4,3-alpyrazin-7(8H)-yl]-1-(2,4,4-trifluorophenyl)butan-2-amine. In an embodiment the invention disclosed polymorphic forms of formula (I), phosphate salt of formula (I) and also a Dibenzoyl-L-tartaric acid salt of formula (I).