CAS: 764667-65-4; 1-(3-(Trifluoromethyl)-5,6-Dihydro-[1,2,4]Triazolo[4,3-A]Pyrazin-7(8H)-yl)-4-(2,4,5-Trifluorophenyl)Butane-1,3-Dione

上下游产品

西他列汀 Sitagliptin 486460-32-6
3-Oxo-3-[3-(Trifluoromethyl)-5,6-Dihydro[1,2,4]Triazolo[4,3-A]Pyrazin-7(8H)-Yl]Propanenitrile
3-(三氟甲基)-5,6,7,8-四氢-[1,2,4]三唑并[4,3-A]吡嗪 3-Trifluoromethyl-5,6,7,8-Tetrahydro-[1,2,4]Triazolo[4,3-A]Pyrazine 486460-21-3

西他列汀置于硫酸,Sodium Nitrite,Potassium Dichromate体系中,化学反应生成 (2Z)-4-氧代-4-[3-(三氟甲基)-5,6-二氢-[1,2,4]三唑并[4,3-A]吡嗪-7-(8H)-基]-1-(2,4,5-三氟苯基)丁-2-酮
参考文献:Drug Derivatives
标题:Drug Derivatives
摘要:本发明涉及已知活性药物化合物的衍生物.这些衍生物通过是活性化合物的氧化还原衍生物与母体活性化合物相区别.这意示活性化合物中的一个或多个官能团已转化为另一组,在一项或多项反应中,这可以被认为代表氧化态的变化.我们通常将这些化合物称为氧化还原衍生物.发明中的衍生物可能与原始母体活性药物化合物仅通过单一步骤转换有关,或者可能通过包括一个或多个氧化态变化的几个合成步骤与之相关.在某些情况下,经过两个或更多转换后获得的官能团可能与母体活性化合物处于相同的氧化态(我们将这些化合物包括在我们的氧化还原衍生物定义中).在其他情况下,发明的衍生物的氧化态可以被认为是与母体化合物不同的.在许多情况下,发明中的化合物本身就具有固有的治疗活性.在某些情况下,相对于母体化合物的相同靶点或靶点,这种活性与母体化合物针对该靶点或靶点的活性一样好或更好.

专利信息

专利号:US-11965193-B2
优先权日:2017-07-11
标题:Use of stereoselective transaminase in asymmetric synthesis of chiral amine
发明人：CHENG ZHANBING; ZHANG TAO; TIAN ZHENHUA; DING SHAONAN
权利人:ABIOCHEM BIOTECHNOLOGY CO LTD
摘要:Use of a stereoselective transaminase in the asymmetric synthesis of a chiral amine. In particular, provided is use of a polypeptide in the production of a chiral amine or a downstream product using a chiral amine as a precursor. Further provided is a method for producing a chiral amine, comprising culturing a strain expressing the polypeptide so as to obtain a chiral amine. Further provided are novel prochiral compounds, a chiral amine production strain and a method for constructing the chiral amine production strain. The stereoselective transaminase has a broad substrate spectrum and thus has a broad application potential in the preparation of a chiral amine.

专利号:WO-2019058290-A1
优先权日:2017-09-20
标 题 :IMPROVED PROCESS FOR THE PREPARATION OF AZANIMOD A-AMINO COMPOUND
发明人：CHINNAPILLAI RAJENDIRAN; PERIYANDI NAGARAJAN; JASTI VENKATESWARALU
权利人:SUVEN LIFE SCIENCES LTD; CHINNAPILLAI RAJENDIRAN; PERIYANDI NAGARAJAN; JASTI VENKATESWARALU
摘要:The present invention relates to an improved process for the preparation of an optically active chiral amino compound. The present invention relates in particular to an improved process for the preparation of (S) -1-amino-2,3-dihydro-1H-indene-4-carbonitrile, an important intermediate for the synthesis of ozanimod. The present invention relates more particularly to the preparation of (S) -1-amino-2,3-dihydro-1H-indene-4-carbonitrile using 4-cyano-1-indanone and alpha-methylbenzylamine derivatives. as raw materials. The present invention particularly relates to the preparation of (S) -1-amino-2,3-dihydro-1H-indene-4-carbonitrile comprising a synthesis of diastereoselective chiral amine by protection with chiral auxiliary ï?¡-methyl benzylamine derivatives followed reduction and debenzylation.

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-9938282-B2
优先权日:2014-02-05
标 题:Expedient synthesis of sitagliptin
发明人：JANAGANI SATYANARAYANA; THADURI VENKATESHWAR KUMAR; VAMARAJU RAVISANKAR
权利人:STEREOKEM INC
摘要:Novel intermediates are disclosed as intermediates for preparation of a Sitagliptin. A novel synthetic method to prepare Sitagliptin using the said intermediates is also disclosed.