Pharmacomodulation on the 3-acetylursolic acid skeleton: Design, synthesis, and biological evaluation of novel N-{3-[4-(3-aminopropyl)piperazinyl]propyl}-3-O-acetylursolamide derivatives as antimalarial agents. Reactions are generally faster in DCE than in THF, and in both solvents, reactions are faster in the presence of AcOH. The amine is acetylated in the third step to form the solid amide in an overall yield of 90%. Efficient one-pot synthesis of N-ethyl amino acids. Highly diastereoselective ortho-lithiation of chiral ferrocenecarboxamides. Synthesis and in vitro activity of new oxazolidinone antibacterial agents having substituted isoxazoles. A fluorescent AND logic gate driven by electrons and protons. A. Todorovic, J. R. Holder, J. W. Scott, C. Haskell-Luevano. Asymmetric synthesis of 4-substituted prolines as conformationally constrained amino acid analogues. Evidence for shape selectivity in non-covalently imprinted polymers. Janine Cossy, Ludovic Tresnard, Domingo Gomez Pardo. Hironori Fukumoto, Keisuke Takahashi, Jun Ishihara, Susumi Hatakeyama. Nicoletta Cini, Elisa Danieli, Gloria Menchi, Andrea Trabocchi, Anna Bottoncetti, Silvia Raspanti, Alberto Pupi, Antonio Guarna. Clay and clay-supported reagents in organic synthesis. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Benoît Blank, Stefan Michlik, Rhett Kempe. Synthesis of Tetrahydropyridoimidazole-2-acetates: Effect of Carboxy and Methoxycarbonyl Groups at C(2) on the Inhibition of Some?- and?-Glycosidases. Liang Yu, Rihui Cao, Wei Yi, Qin Yan, Zhiyong Chen, Lin Ma, Wenlie Peng, Huacan Song. Part 1: Discovery and initial structure–activity relationships for 1-amino-2-phenyl-4-(piperidin-1-yl)butanes. Uta Funke, Steffen Fischer, Achim Hiller, Matthias Scheunemann, Winnie Deuther-Conrad, Peter Brust, Jörg Steinbach. Synthesis of [ 3-Aza-6,8-dioxabicyclo[3.2.1]octanes as new enantiopure heteroatom-rich tropane-like ligands of human dopamine transporter. From Molecular Shape to Potent Bioactive Agents II: Fragment‐Based de novo Design. Michael W. Miller, Susan F. Vice, Stuart W. McCombie. Sodium triacetoxyborohydride (STAB) is a common reducing agent for reductive aminations. Heshmatollah Alinezhad, Mahmood Tajbakhsh, Nastaran Mahdavi. under 1 MPa. It was found that the yield of secondary amine depends on the rate of formation of intermediate imine. Potent and selective thrombin inhibitors featuring hydrophobic, basic P3P4-aminoalkyllactam moieties. Synthetic studies towards ML-3000 a concise synthesis of this non-steroidal anti-inflammatory drug. Reductive Amination of Aldehydes and Ketones in a Heterogeneous System in THF and under Solvent-Free Conditions Using Sodium Borohydride-Silica Phosphoric Acid. Sodium triacetoxyborohydride was successfully used in the reductive amination of variety of aldehydes and ketones with primary and secondary amines. Parallel modification of tropane alkaloids. Guoping Xue, Jerald S Bradshaw, N.Kent Dalley, Paul B Savage, Krzysztof E Krakowiak, Reed M Izatt, Luca Prodi, Marco Montalti, Nelsi Zaccheroni. Microwave-Promoted Selective Mono-N-Alkylation of Anilines with Tertiary Amines by Heterogeneous Catalysis. 3 Michele Stabile-Harris, April Ciampoli. Corinne Soulié, Pierre Bassoul, François Tournilhac. Nan Zheng, Joseph D. Armstrong, Kan K. Eng, Jennifer Keller, Tom Liu, Robert Purick, Joseph Lynch, Frederick W. Hartner, R.P. Fluorescence labelling of carbohydrates with 2-aminobenzamide (2AB). Direct and indirect reductive amination of aldehydes and ketones with solid acid-activated sodium borohydride under solvent-free conditions. Selective one-pot synthesis of symmetrically and unsymmetrically substituted amines via rhodium catalysed multiple alkylations of ammonia or primary amines under hydroformylation conditions. Kuan-Liang Wei, Jeng-Yue Wu, Yu-Min Chen, Yen-Chi Hsu, Jiang-Jen Lin. On the importance of the pore inner cavity for the ionophoric activity of 1,3-alternate calix[4]arene/steroid conjugates. A Simple Stereoselective Route to α-Trifluoromethyl Analogues of Piperidine Alkaloids. Stereoselective synthesis and structure–affinity relationships of bicyclic κ receptoragonists. The dynamic nature of the imine as well as the versatility of reductive amination to functionalize a polymer with a range of amino acids is highlighted. Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists. A convenient method for producing radioiodinated compounds in high effective specific activity. Georg Dirscherl, Robert Knape, Paul Hanson, Burkhard König. Polymer-supported triacetoxyborohydride: a novel reagent of choice for reductive amination. Raymond Luguya, Laurent Jaquinod, Frank R Fronczek, M.Graça H Vicente, Kevin M Smith. Solid-phase extraction on C18 silica as a purification strategy in the solution synthesis of a 1-thio-β- d -galactopyranoside library. 3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinoline-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: Chemical synthesis, evaluation in vitro and radiofluorination. Savage, Guo-Ping Xue, Joseph A. Chiara, Reed M. Izatt, Jerald S. Bradshaw, Krzysztof E. Krakowiak. Ryoichi Hiroi, Norikazu Miyoshi, Makoto Wada. Scott E. Watkins, Donald C. Craig, Stephen B. Colbran. Specific Radiopharmaceuticals. Novel functionalized pyridine-containing DTPA-like ligand. 7H P[(S,S,S)-CH3NCH(CH2Ph)CH2]3N: a new C3-symmetric enantiomerically pure proazaphosphatrane. STAB is H2O sensitive and not very compatible with MeOH, therefore reactions are typically done in other solvents (ex. We present a reductive amination experiment for a second-semester organic chemistry class. 2A Agustin Casimiro-Garcia, Erik De Clercq, Christophe Pannecouque, Myriam Witvrouw, Tracy L Loftus, Jim A Turpin, Robert W Buckheit, Phillip E Fanwick, Mark Cushman. In comparison with other reductive amination procedures such as NaBH(3)CN/MeOH, borane-pyridine, and catalytic hydrogenation, NaBH(OAc)(3) gave consistently higher yields and fewer side products. A slurry of the amine (50 mg, 0.12 mmol) and the aldehyde (31.6 mg, 0.18 mmol) in 1,4-Dioxane (3 mL) was stirred for 5 min then treated with NaBH (OAc)3 (77 mg, 0.363 mmol). Zhong-Zheng Zhou, Wei Huang, Feng-Qin Ji, Ming-Wu Ding, Guang-Fu Yang. Noteworthy is that highly chemoselective reactions were achieved with the co-existence of other functionalities such as halogen, carbon-carbon double bond and hydroxyl groups. Journal of Polymer Science Part A: Polymer Chemistry. Synthesis of heterocycles via ligand-free palladium catalyzed reductive Heck cyclization. 4-[(8-Alkyl-8-azabicyclo[3.2.1]octyl-3-yl)-3-arylanilino]- N , N -diethylbenzamides: high affinity, selective ligands for the delta opioid receptor illustrate factors important to antagonist activity. A mixture of the amine (193 mg, 0.727 mmol), aldehyde (200 mg, 0.56 mmol), and TEA (0.074 g, 0.727 mmol) were stirred in 5% AcOH in DMF for 30 min. Proteins: Structure, Function, and Bioinformatics. An efficient conversion of nitroaromatics and aromatic amines to tertiary amines in one-pot way. Water was removed by azeotropic distillation using a Dean-Stark trap. four classes based on the functionality of their side chains (acidic, polar neutral, neutral and basic) and use their amine groups in condensation reactions with aldehyde functional polymers. Britta C. Sasse, Ulrich R. Mach, Jukka Leppaenen, Thierry Calmels, Holger Stark. Heshmat Alinezhad, Mahmood Tajbakhsh, Fatemeh Salehian, Kazem Fazli. Jason J. Chruma, Dalibor Sames, Robin Polt. Organocatalytic Conjugate Addition of Malonates to α,β-Unsaturated Aldehydes: Asymmetric Formal Synthesis of (−)-Paroxetine, Chiral Lactams, and Lactones. Acetoacetoxy ethyl methacrylate (AAEM) resin, a new scavenger for primary amines in the presence of secondary amines. Moslem M. Lakouraj, Mahmood Tajbakhsh, Majid S. Mahalli. All rights reserved. Solid phase synthesis of 6-acylamino-1-alkyl/aryl-4-oxo-1,4-dihydrocinnoline-3-carboxamides. Annabelle Bariau, Wahid Bux Jatoi, Pierre Calinaud, Yves Troin, Jean-Louis Canet. K. Shankaran, Karla L. Donnelly, Shrenik K. Shah, Charles G. Caldwell, Ping Chen, Paul E. Finke, Bryan Oates, Malcolm MacCoss, Sander G. Mills, Julie A. DeMartino, Sandra L. Gould, Lorraine Malkowitz, Salvatore J. Siciliano, Martin S. Springer, Gloria Kwei, Anthony Carella, Gwen Carver, Renee Danzeisen, Daria Hazuda, Karen Holmes, Joseph Kessler, Janet Lineberger, Michael D. Miller, Emilio A. Emini, William A. Schleif. Synthesis and evaluation of a new class of tertiary alcohol based BACE-1 inhibitors. Sodium triacetoxyborohydride is presented as a general reducing agent for the reductive amination of aldehydes and ketones. A selective reductive amination of aldehydes by the use of Hantzsch dihydropyridines as reductant. Microwave-accelerated reductive amination between ketones and ammonium acetate. Fanny Chaux, Franck Denat, Enrique Espinosa, Roger Guilard. In this experiment, students react a selection of benzylamines with aldehydes to form the corresponding imines. Gallium(III) Triflate Catalyzed Direct Reductive Amination of Aldehydes. Li Dong, Saadat Aleem, Cynthia A. Fink. S. Ghanbari Pakdehi, G. Abolhamd, M. Sohrabi, A. Saberi Moghaddam, A. Zarei. Request the article directly from the authors on ResearchGate. Synthetic medicinal chemistry of selected antimalarial natural products. Zhibo Zhang, Satu Mikkola, Harri Lonnberg. Peptide- or Protein-Cleaving Agents Based on Metal Complexes. Paul E Finke, Laura C Meurer, Bryan Oates, Sander G Mills, Malcolm MacCoss, Lorraine Malkowitz, Martin S Springer, Bruce L Daugherty, Sandra L Gould, Julie A DeMartino, Salvatore J Siciliano, Anthony Carella, Gwen Carver, Karen Holmes, Renee Danzeisen, Daria Hazuda, Joseph Kessler, Janet Lineberger, Michael Miller, William A Schleif, Emilio A Emini. Synthesis and activity of the melanocortin Xaa-d-Phe-Arg-Trp-NH2 tetrapeptides with amide bond modifications. ZrCl4/Hantzsch 1,4-dihydropyridine as a new and efficient reagent combination for the direct reductive amination of aldehydes and ketones with weakly basic amines. Ewgenij Proschak, Kerstin Sander, Heiko Zettl, Yusuf Tanrikulu, Oliver Rau, Petra Schneider, Manfred Schubert‐Zsilavecz, Holger Stark, Gisbert Schneider. The first step is a spectacular solvent-free solid-solid reaction between ortho-vanillin and para-toluidine to synthesize an imine in quantitative yield. Regis Vanderesse, Laurent Thevenet, Michel Marraud, Nicole Boggetto, Michele Reboud, Catherine Corbier. Mayur J. Bhanushali, Nitin S. Nandurkar, Malhari D. Bhor, Bhalchandra M. Bhanage. Bruhaspathy Miriyala, Sukanta Bhattacharyya, John S Williamson. Farajollah Mohanazadeh, Mehdi Forozani, Azam Taheri. II. A simple flowcell for reaction monitoring by NMR. and 5-HT Sukanta Bhattacharyya, Arindam Chatterjee, John S. Williamson. Reductive Aminations of Carbonyl Compounds with Borohydride and Borane Reducing Agents. David Blomberg, Tomas Fex, Yafeng Xue, Kay Brickmann, Jan Kihlberg. A convenient one pot synthesis of fentanyl. Sodium triacetoxyborohydride is a reagent of choice in the reductive amination of aldehydes and saturated aliphatic ketones with primary and secondary amines. Synthesis of polyfunctional quinolizidine alkaloids: development towards selective glycosidase inhibitors. Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Chingakham B. Singh, Veerababurao Kavala, Akshaya K. Samal, Bhisma K. Patel. The residue was purified by silica gel flash chromatography to provide the product. Studies on Direct and Indirect Reductive Amination Procedures.. Jotham W Coe, Michael G Vetelino, Michael J Bradlee. DCE, DCM, THF, or dioxane). Nadia Patino, Christophe Di Giorgio, Cristina Dan-Covalciuc, Valérie Peytou, Raphaël Terreux, Daniel Cabrol-Bass, Christian Bailly, Roger Condom. The effect of substituents on the feasibility of azomethine-azomethine isomerization: New synthetic opportunities for biomimetic transamination. NMR spectroscopy clearly indicates that the nuclei of the methyl groups (and the hydrogens of each methylene) of 2 and 3 are enantiotopic and diastereotopic, respectively.

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