CAS: 1538-08-5; 2,2,2-Trifluoroacetohydrazide

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3082507-62-5 22547-51-9 2361643-91-4

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2,2,2-三氟乙酰胺 2,2,2-Trifluoroacetamide 354-38-1

三氟乙酸乙酯置于hydrazine Hydrate体系中,用 乙腈 用作溶剂,以69.5%的收率获得三氟乙酰肼
参考文献:新型三唑并[4,3-A]吡嗪类似物的设计,合成,生物学评价和计算研究
标题:新型三唑并[4,3-A]吡嗪类似物的设计,合成,生物学评价和计算研究
摘要:摘要 三唑并 [4,3-A] 吡嗪类似物因其对各种传染性和非传染性疾病的潜在活性而受到关注.为了寻找合适的有效候选药物,我们在此报告了新型三唑并 [4,3-A] 吡嗪类似物的设计,合成,表征,生物活性和计算研究.合成的分子通过各种光谱研究进行表征,如红外,质谱,1H NMR,13C NMR 和元素分析.评估了新合成的化合物的体外生物活性,例如分别对恶性疟原虫,H37Rv,各种细菌和真菌菌株的抗疟疾,抗结核,抗菌和抗真菌活性.用来自恶性疟原虫的酶天冬氨酸蛋白酶酶原 Proplasmepsin Ii 进行分子对接研究,以分析它们在天冬氨酸蛋白酶活性位点的结合方向.对最佳对接复合物进行分子动力学模拟,以说明这些复合物的稳定性以及模拟轨迹期间最突出的相互作用.我们还计算了所有合成化合物的 Admet 特性,以预测用于选择化合物活性和生物利用度的药代动力学特性.对最佳对接复合物进行分子动力学模拟,以
Doi:10.1016/j.Molstruc.2019.01.091

专利信息

专利号:US-10640508-B2
优先权日:2017-10-13
标 题 :Diazene directed modular synthesis of compounds with quaternary carbon centers
发明人：MOVASSAGHI MOHAMMAD; LINDOVSKA PETRA
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Diazene-directed modular synthesis is described for the preparation Csp2-Csp3 and Csp3-Csp3 linkages where one or more stereogenic quaternary carbon centers are formed. The disclosed methods are directed to the preparation of compounds of Formula (I), or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, from compounds of Formula (II): n nwherein R 1 -R 5 and q are as defined independently for each occurrence herein. A wide variety of compounds can be accessed in this manner, including oligocyclotryptamines, where the stereochemistry of each subunit is beneficially secured before fragment coupling.

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:EP-1058678-B1
优先权日:1998-02-26
标 题:Metal-catalyzed arylations and vinylations of hydrazines, hydrazones, hydroxylamines and oximes
发明人：BUCHWALD STEPHEN L; WAGAW SEBLE; GEIS OLIVER
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.

专利号:US-7495123-B2
优先权日:2004-04-05
标 题:Process for the preparation of enantiomerically enriched beta amino acid derivatives
发明人：XIAO YI; SUN YONGKUI; ROSNER THORSTEN; RIVERA NELO R; KRSKA SHANE W; CLAUSEN ANDREW M; ARMSTRONG III JOSEPH D; SPINDLER FELIX; MALAN CHRISTOPHE
权利人:SOLVIAS AG; MERCK & CO INC
摘要:The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.

专利号:US-11225655-B2
优先权日:2010-04-16
标题:Bi-functional complexes and methods for making and using such complexes
发明人：GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK
权利人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK; NUEVOLUTION AS
摘要:The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.

专利号:EP-1222172-A1
优先权日:1999-10-21
标题 :Synthesis of 1,3,5-trisubstituted pyrazoles and intermediates therefore