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2023
Base-mediated homologative rearrangement of nitrogen-oxygen bonds of N-methyl-N-oxyamides
Malik, M., Senatore, R., Langer, T., Holzer, W. & Pace, V., 29 Aug 2023, In: Chemical Science. 14, 37, p. 10140-10146 7 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Design, synthesis and preclinical evaluation of muscarine receptor antagonists via a scaffold-hopping approach
Millard, M., Kilian, J., Ozenil, M., Mogeritsch, M., Schwingenschlögl-Maisetschläger, V., Holzer, W., Hacker, M., Langer, T. & Pichler, V., 15 Dec 2023, In: European Journal of Medicinal Chemistry. 262, 115891.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
2022
Design, Synthesis, and Biological Evaluation of 4,4’-Difluorobenzhydrol Carbamates as Selective M1 Antagonists
Kilian, J., Ozenil, M., Millard, M., Fürtös, D., Maisetschläger, V., Holzer, W., Wadsak, W., Hacker, M., Langer, T. & Pichler, V., Feb 2022, In: Pharmaceuticals. 15, 2, 18 p., 248.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Straightforward synthesis of bench-stable heteroatom-centered difluoromethylated entities via controlled nucleophilic transfer from activated TMSCHF 2.
Miele, M., Castoldi, L., Simeone, X., Holzer, W. & Pace, V., 2022, In: Chemical Communications. 58, 38, p. 5761-5764 4 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Synthesis, Biological Evaluation, and Docking Studies of Antagonistic Hydroxylated Arecaidine Esters Targeting mAChRs
Kilian, J., Millard, M., Ozenil, M., Krause, D., Ghaderi, K., Holzer, W., Urban, E., Spreitzer, H., Wadsak, W., Hacker, M., Langer, T. & Pichler, V., May 2022, In: Molecules. 27, 10, 21 p., 3173.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
2021
A 13C chemical shifts study of iodopyrazoles: experimental results and relativistic and non-relativistic calculations
Alkorta, I., Claramunt, R. M., Sanz, D., Elguero, J. & Holzer, W., Jun 2021, In: Structural Chemistry. 32, 3, p. 925-937 13 p.Publications: Contribution to journal › Article › Peer Reviewed
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Consecutive and Selective Double Methylene Insertion of Lithium Carbenoids to Isothiocyanates: A Direct Assembly of Four-Membered Sulfur-Containing Cycles
Senatore, R., Malik, M., Langer, T., Holzer, W. & Pace, V., 15 Nov 2021, In: Angewandte Chemie - International Edition. 60, 47, p. 24854-24858 5 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Direct and straightforward transfer of C1 functionalized synthons to phosphorous electrophiles for accessinggem-P-containing methanes
Touqeer, S., Ielo, L., Miele, M., Urban, E., Holzer, W. & Pace, V., 21 Mar 2021, In: Organic and Biomolecular Chemistry. 19, 11, p. 2425-2429 5 p.Publications: Contribution to journal › Article › Peer Reviewed
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Pseudo-Dipeptide Bearing alpha,alpha-Difluoromethyl Ketone Moiety as Electrophilic Warhead with Activity against Coronaviruses
Citarella, A., Gentile, D., Rescifina, A., Piperno, A., Mognetti, B., Gribaudo, G., Sciortino, M. T., Holzer, W., Pace, V. & Micale, N., 2 Feb 2021, In: International Journal of Molecular Sciences. 22, 3, p. 1-17 17 p., 1398.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Synthesis of stable α-fluoromethyl putative carbanions via a chemoselective reduction-monofluoromethylation sequence of diselenides under sustainable conditions
Senatore, R., Malik, M., Urban, E., Holzer, W. & Pace, V., 9 Apr 2021, In: Tetrahedron. 85, 8 p., 131921.Publications: Contribution to journal › Article › Peer Reviewed
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Taking advantage of lithium monohalocarbenoid intrinsic α-elimination in 2-MeTHF: controlled epoxide ring-openingen routeto halohydrins
Ielo, L., Miele, M., Pillari, V., Senatore, R., Mirabile, S., Gitto, R., Holzer, W., Alcántara, A. R. & Pace, V., 7 Mar 2021, In: Organic and Biomolecular Chemistry. 19, 9, p. 2038-2043 6 p.Publications: Contribution to journal › Article › Peer Reviewed
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Unexpected scaffold rearrangement product of pirenzepine found in commercial samples
Ozenil, M., Skos, L., Roller, A., Gajic, N., Holzer, W., Spreitzer, H., Platzer-Ozenil, S., Vraka, C., Hacker, M., Wadsak, W. & Pichler, V., 3 Dec 2021, In: Scientific Reports. 11, 1, 10 p., 23397.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
2020
Chemoselective Homologation-Deoxygenation Strategy Enabling the Direct Conversion of Carbonyls into (n+1)-Halomethyl-Alkanes
Miele, M., Citarella, A., Langer, T., Urban, E., Zehl, M., Holzer, W., Ielo, L. & Pace, V., 2 Oct 2020, In: Organic Letters. 22, 19, p. 7629-7634 6 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Consecutive C1-Homologation / Displacement Strategy for Converting Thiosulfonates into O,S-Oxothioacetals
Ielo, L., Pillari, V., Miele, M., Holzer, W. & Pace, V., 8 Dec 2020, In: Advanced Synthesis and Catalysis. 362, 23, p. 5444-5449 6 p.Publications: Contribution to journal › Article › Peer Reviewed
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Direct and Chemoselective Electrophilic Monofluoromethylation of Heteroatoms (O-, S-, N-, P-, Se-) with Fluoroiodomethane
Senatore, R., Malik, M., Spreitzer, M., Holzer, W. & Pace, V., 21 Feb 2020, In: Organic Letters. 22, 4, p. 1345-1349 5 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Electrophilicity Scale of Activated Amides: 17O NMR and 15N NMR Chemical Shifts of Acyclic Twisted Amides in N−C(O) Cross-Coupling
Ielo, L., Pace, V., Holzer, W., Rahman, M. M., Meng, G., Szostak, R. & Szostak, M., 9 Dec 2020, In: Chemistry: A European Journal. 26, 69, p. 16246-16250 5 p.Publications: Contribution to journal › Article › Peer Reviewed
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Enhanced arecoline derivatives as muscarinic acetylcholine receptor M1 ligands for potential application as PET radiotracers
Ozenil, M., Pacher, K., Balber, T., Vraka, C., Roller, A., Holzer, W., Spreitzer, H., Mitterhauser, M., Wadsak, W., Hacker, M. & Pichler, V., 15 Oct 2020, In: European Journal of Medicinal Chemistry. 204, 18 p., 112623.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Halogen-Imparted Reactivity in Lithium Carbenoid Mediated Homologations of Imine Surrogates: Direct Assembly of bis-Trifluoromethyl-β-Diketiminates and the Dual Role of LiCH 2I
Ielo, L., Castoldi, L., Touqeer, S., Lombino, J., Roller, A., Prandi, C., Holzer, W. & Pace, V., 16 Nov 2020, In: Angewandte Chemie (International Edition). 59, 47, p. 20852-20857 6 p.Publications: Contribution to journal › Article › Peer Reviewed
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Straightforward and direct access to β-seleno- amines and sulfonylamides via the controlled addition of phenylselenomethyllithium (LiCH2SePh) to imines
Senatore, R., Malik, M., Touqeer, S., Listro, R., Collina, S., Holzer, W. & Pace, V., 18 Dec 2020, In: Tetrahedron. 76, 51, 11 p., 131220.Publications: Contribution to journal › Article › Peer Reviewed
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Straightforward chemoselective access to unsymmetrical dithioacetals through a thiosulfonate homologation-nucleophilic substitution sequence
Ielo, L., Pillari, V., Gajic, N., Holzer, W. & Pace, V., 21 Oct 2020, In: Chemical Communications. 56, 82, p. 12395-12398 4 p.Publications: Contribution to journal › Article › Peer Reviewed
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Synthesis, Biological, and Computational Evaluation of Antagonistic, Chiral Hydrobenzoin Esters of Arecaidine Targeting mAChR M1
Ozenil, M., Aronow, J., Piljak, D., Vraka, C., Holzer, W., Spreitzer, H., Wadsak, W., Hacker, M. & Pichler, V., 30 Nov 2020, In: Pharmaceuticals. 13, 12, p. 1-12 12 p., 437.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Synthesis and anthelmintic activity of benzopyrano[2,3-c]pyrazol-4(2H)-one derivatives
Milišiūnaitė, V., Kadlecová, A., Žukauskaitė, A., Doležal, K., Strnad, M., Voller, J., Arbačiauskienė, E., Holzer, W. & Šačkus, A., 1 Nov 2020, In: Molecular Diversity. 24, 4, p. 1025-1042 18 p.Publications: Contribution to journal › Article › Peer Reviewed
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2019
17O NMR and 15N NMR chemical shifts of sterically-hindered amides: Ground-state destabilization in amide electrophilicity
Pace, V., Holzer, W., Ielo, L., Shi, S., Meng, G., Hanna, M., Szostak, R. & Szostak, M., 1 Jan 2019, In: Chemical Communications. 55, 30, p. 4423-4426 4 p.Publications: Contribution to journal › Article › Peer Reviewed
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A Straightforward Homologation of Carbon Dioxide with Magnesium Carbenoids en Route to α-Halocarboxylic Acids
Monticelli, S., Urban, E., Langer, T., Holzer, W. & Pace, V., 5 Mar 2019, In: Advanced Synthesis & Catalysis. 361, 5, p. 1001-1006 6 p.Publications: Contribution to journal › Article › Peer Reviewed
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Chemoselective reduction of isothiocyanates to thioformamides mediated by the Schwartz reagent
De La Vega-Hernández, K., Senatore, R., Miele, M., Urban, E., Holzer, W. & Pace, V., 1 Jan 2019, In: Organic and Biomolecular Chemistry. 17, 7, p. 1970-1978 9 p.Publications: Contribution to journal › Article › Peer Reviewed
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Design, Synthesis, and Pharmacological Evaluation of Novel β2/3 Subunit-Selective γ-Aminobutyric Acid Type A (GABA A ) Receptor Modulators
Stadler, M., Monticelli, S., Seidel, T., Luger, D., Salzer, I., Boehm, S., Holzer, W., Schwarzer, C., Urban, E., Khom, S., Langer, T., Pace, V. & Hering, S., 1 Oct 2019, In: Journal of Medicinal Chemistry. 62, 1, p. 317-341 25 p.Publications: Contribution to journal › Article › Peer Reviewed
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Direct and Chemoselective Synthesis of Tertiary Difluoroketones via Weinreb Amide Homologation with a CHF2-Carbene Equivalent
Miele, M., Citarella, A., Micale, N., Holzer, W. & Pace, V., 18 Oct 2019, In: Organic Letters. 21, 20, p. 8261-8265 5 p.Publications: Contribution to journal › Article › Peer Reviewed
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Highly chemoselective difluoromethylative homologation of iso(thio)cyanates: Expeditious access to unprecedented α,α-difluoro(thio)amides
Miele, M., D'Orsi, R., Sridharan, V., Holzer, W. & Pace, V., 1 Jan 2019, In: Chemical Communications. 55, 86, p. 12960-12963 4 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Modular and Chemoselective Strategy for the Direct Access to a-Fluoropoxides and Aziridines via the Addition of Fluoroiodomethyllithium to Carbonyl-Like Compounds
Monticelli, S., Colella, M., Pillari, V., Tota, A., Langer, T., Holzer, W., Degennaro, L., Luisi, R. & Pace, V., 2019, p. 584-588.Publications: Contribution to conference › Paper › Peer Reviewed
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Modular and Chemoselective Strategy for the Direct Access to α-Fluoroepoxides and Aziridines via the Addition of Fluoroiodomethyllithium to Carbonyl-Like Compounds
Monticelli, S., Colella, M., Pillari, V., Tota, A., Langer, T., Holzer, W., Degennaro, L., Luisi, R. & Pace, V., 18 Jan 2019, In: Organic Letters. 21, 2, p. 584-588 5 p.Publications: Contribution to journal › Article › Peer Reviewed
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Multinuclear NMR spectra and GIAO/DFT calculations of N-benzylazoles and N-benzylbenzazoles
Holzer, W., Castoldi, L., Kyselova, V., Sanz, D., Claramunt, R. M., Torralba, M. C., Alkorta, I. & Elguero, J., 1 Oct 2019, In: Structural Chemistry. 30, 5, p. 1729-1735 7 p.Publications: Contribution to journal › Article › Peer Reviewed
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Separating chromatographically indistinguishable diaxial from diequatorial disaccaride azidonitrales, comprises e.g. treating mixture of the diaxial and diequatorial azidonitrates with nucleophile, preferably tetraalkylammonium nitrate
Unger, F., Viernstein, H., Holzer, W. & Midpanon, S., 2019Publications: Patent
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Sustainable Asymmetric Organolithium Chemistry: Enantio- and Chemoselective Acylations through Recycling of Solvent, Sparteine, and Weinreb "Amine"
Monticelli, S., Holzer, W., Langer, T., Roller, A., Olofsson, B. & Pace, V., 21 Mar 2019, In: ChemSusChem. 12, 6, p. 1147-1154 8 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Sustainable Asymmetric Organolithium Chemistry: Enantio-and Chemoselective Acylation through Recycling of Solvent, Sparteine and Weinred "Amine"
Monticelli, S., Holzer, W., Langer, T., Roller, A., Olofsson, B. & Pace, V., 2019.Publications: Contribution to conference › Paper › Peer Reviewed
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Synthesis of 2H-furo[2,3-c]pyrazole ring systems through silver(I) ion-mediated ring-closure reaction
Milišiūnaitė, V., Paulavičiūtė, R., Arbačiauskienė, E., Martynaitis, V., Holzer, W. & Šačkus, A., 14 Mar 2019, In: Beilstein Journal of Organic Chemistry. 15, p. 679-684 6 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Telescoped, Divergent, Chemoselective C1 and C1-C1 Homologation of Imine Surrogates: Access to Quaternary Chloro- and Halomethyl-Trifluoromethyl Aziridines
Ielo, L., Touqeer, S., Roller, A., Langer, T., Holzer, W. & Pace, V., 18 Feb 2019, In: Angewandte Chemie (International Edition). 58, 8, p. 2479-2484 6 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
2018
An unusual thionyl chloride-promoted C-C bond formation to obtain 4,4 '-bipyrazolones
Eller, G. A., Vilkauskaite, G., Sackus, A., Martynaitis, V., Mamuye, A. D., Pace, V. & Holzer, W., 4 Jun 2018, In: Beilstein Journal of Organic Chemistry. 14, p. 1287-1292 6 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Expeditious and Chemoselective Synthesis of α-Aryl and α-Alkyl Selenomethylketones via Homologation Chemistry
Senatore, R., Castoldi, L., Ielo, L., Holzer, W. & Pace, V., 4 May 2018, In: Organic Letters. 20, 9, p. 2685-2688 4 p.Publications: Contribution to journal › Article › Peer Reviewed
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Homologation of halostannanes with carbenoids: a convenient and straightforward one-step access to α-functionalized organotin reagents
Touqeer, S., Castoldi, L., Langer, T., Holzer, W. & Pace, V., 6 Sept 2018, In: Chemical Communications. 54, 72, p. 10112-10115 4 p.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Merging lithium carbenoid homologation and enzymatic reduction: A combinative approach to the HIV-protease inhibitor Nelfinavir
Castoldi, L., Ielo, L., Hoyos, P., Hernaiz, M. J., De Luca, L., Alcantara, A. R., Holzer, W. & Pace, V., 3 May 2018, In: Tetrahedron. 74, 18, p. 2211-2217 7 p.Publications: Contribution to journal › Article › Peer Reviewed
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One-pot synthesis of polycyclic heterocyclic compounds by condensation of 1-carbamoylmethyl-2,3,3-trimethyl-3H-indolium salts with pyridine-2, 3, and 4-and quinoline-4-carboxaldehydes
Sackus, A., Zukauskaite, Z., Kleiziene, N., Bieliauskas, A., Amankaviciene, V., Holzer, W. & Martynaitis, V., 5 Jul 2018, In: Tetrahedron. 74, 27, p. 3679-3690 12 p.Publications: Contribution to journal › Article › Peer Reviewed
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On the Tautomerism of N-Substituted Pyrazolones: 1,2-Dihydro-3H-pyrazol-3-ones versus 1H-Pyrazol-3-ols
Arbaciauskiene, E., Krikstolaityte, S., Mitruleviciene, A., Bieliauskas, A., Martynaitis, V., Bechmann, M., Roller, A., Sackus, A. & Holzer, W., Jan 2018, In: Molecules. 23, 1, 15 p., 129.Publications: Contribution to journal › Article › Peer Reviewed
Open Access -
Prebiotic composition used as food supplement or functional food, and to prevent or treat inflammatory bowel diseases, comprises oligosaccharide e.g. beta-glucose-(1,4)(beta-galactose)-(1,2)-alpha-galactose-(1,6))mannose tetrasaccharide
Cavarkapa, A., Holzer, W., Müller, M., Okonogi, S., Praznik, W., Unger, F. & Viernstein, H., 2018Publications: Patent
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Ring-closing metathesis as a key step to construct the 2, 6-dihydropyrano[2, 3-c]pyrazole ring system
Bieliauskas, A., Krikštolaityte, S., Holzer, W. & Šackus, A., 7 Jul 2018, In: ARKIVOC. 5/2018, p. 296-307 12 p.Publications: Contribution to journal › Article › Peer Reviewed
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Substituted α-Sulfur Methyl Carbanions: Effective Homologating Agents for the Chemoselective Preparation of β-Oxo Thioethers from Weinreb Amides
Senatore, R., Ielo, L., Urban, E., Holzer, W. & Pace, V., 7 Jun 2018, In: European Journal of Organic Chemistry. 2018, 20-21, p. 2466-2470 5 p.Publications: Contribution to journal › Article › Peer Reviewed
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Synthesis and anti-mitotic activity of 2,4-or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines
Milisiunaite, V., Arbaciauskiene, E., Reznickova, E., Jorda, R., Malinkova, V., Zukauskaite, A., Holzer, W., Sackus, A. & Krystof, V., 25 Apr 2018, In: European Journal of Medicinal Chemistry. 150, p. 908-919 12 p.Publications: Contribution to journal › Article › Peer Reviewed
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Synthesis and NMR-Spectroscopic Investigations with 4-Chloroacyl-1-phenylpyrazolin-5-ones
Eller, G. A. & Holzer, W., Jan 2018, In: Journal of heterocyclic chemistry. 55, 1, p. 132-137 6 p.Publications: Contribution to journal › Article › Peer Reviewed
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α-Arylamino Diazoketones: Diazomethane-Loading Controlled Synthesis, Spectroscopic Investigations and Structural X-ray Analysis
Castoldi, L., Ielo, L., Holzer, W., Giester, G., Roller, A. & Pace, V., Apr 2018, In: The Journal of Organic Chemistry. 83, 8, p. 4336-4347 12 p.Publications: Contribution to journal › Article › Peer Reviewed
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2017
A greener and efficient access to substituted four- and six-membered sulfur-bearing heterocycles
Parisi, G., Degennaro, L., Carlucci, C., de Candia, M., Mastrorilli, P., Roller, A., Holzer, W., Altomare, C. D., Pace, V. & Luisi, R., 21 Jun 2017, In: Organic & Biomolecular Chemistry. 15, 23, p. 5000-5015 16 p.Publications: Contribution to journal › Article › Peer Reviewed
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Corrigendum: Structures of Highly Twisted Amides Relevant to Amide N-C Cross-Coupling: Evidence for Ground-State Amide Destabilization (vol 22, pg 14496, 2016)
Pace, V., Holzer, W., Meng, G., Shi, S., Lalancette, R., Szostak, R. & Szostak, M., Mar 2017, In: Chemistry: A European Journal. 23, 14, p. 3496-3496 1 p.Publications: Contribution to journal › Correction › Peer Reviewed
Open Access