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1
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Conjugate Addition of Lithiated ( S )‐4‐Isopropyl‐3‐ [(methylthio)methyl]‐5,5‐diphenyloxazolidin‐2‐one to Cinnamoyl Derivatives: Preparation of Enantiomerically Pure 1,4‐Diols

Gaul, Christoph ; Seebach, Dieter

Helvetica Chimica Acta, March 2002, Vol.85(3), pp.772-787 [Peer Reviewed Journal]

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Confirmation of the structures of synthetic derivatives of migrastatin in the light of recently disclosed crystallographically based claims

Nagorny, Pavel ; Krauss, Isaac ; Njardarson, Jón T ; Perez, Lucy ; Gaul, Christoph ; Yang, Guangli ; Ouerfelli, Ouathek ; Danishefsky, Samuel J

Tetrahedron Letters, 2010, Vol.51(30), pp.3873-3875 [Peer Reviewed Journal]

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Synthesis of the macrolide core of migrastatin

Gaul, Christoph ; Danishefsky, Samuel J

Tetrahedron Letters, 2002, Vol.43(50), pp.9039-9042 [Peer Reviewed Journal]

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4
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The total synthesis of (+)-migrastatin

Gaul, Christoph ; Njardarson, Jon T ; Danishefsky, Samuel J

Journal of the American Chemical Society, 21 May 2003, Vol.125(20), pp.6042-3 [Peer Reviewed Journal]

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5
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Synthetic analogues of migrastatin that inhibit mammary tumor metastasis in mice

Shan, Dandan ; Chen, Lin ; Njardarson, Jon T ; Gaul, Christoph ; Ma, Xiaojing ; Danishefsky, Samuel J ; Huang, Xin-Yun

Proceedings of the National Academy of Sciences of the United States of America, 08 March 2005, Vol.102(10), pp.3772-6 [Peer Reviewed Journal]

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En route to the total synthesis of tashironin: on the exercise of stereochemical control by a methyl group in mediating remote cyclization reactions

Cook, Silas P ; Gaul, Christoph ; Danishefsky, Samuel J

Tetrahedron Letters, 2005, Vol.46(5), pp.843-847 [Peer Reviewed Journal]

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Lithiated 4-Isopropyl-3-(methylthiomethyl)-5,5-diphenyloxazolidin-2-one:  A Chiral Formyl Anion Equivalent for Enantioselective Preparations of 1,2-Diols, 2-Amino Alcohols, 2-Hydroxy Esters, and 4-Hydroxy-2-alkenoates
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Lithiated 4-Isopropyl-3-(methylthiomethyl)-5,5-diphenyloxazolidin-2-one:  A Chiral Formyl Anion Equivalent for Enantioselective Preparations of 1,2-Diols, 2-Amino Alcohols, 2-Hydroxy Esters, and 4-Hydroxy-2-alkenoates

Gaul, Christoph ; Schärer, Kaspar ; Seebach, Dieter

The Journal of Organic Chemistry, 05/2001, Vol.66(9), pp.3059-3073 [Peer Reviewed Journal]

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A Valine-Derived Lithiated 3-Methylthiomethyl-1,3-oxazolidin-2-one for Enantioselective Nucleophilic Hydroxymethylation, Formylation, and Alkoxycarbonylation of Aldehydes
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A Valine-Derived Lithiated 3-Methylthiomethyl-1,3-oxazolidin-2-one for Enantioselective Nucleophilic Hydroxymethylation, Formylation, and Alkoxycarbonylation of Aldehydes

Gaul, Christoph ; Seebach, Dieter

Organic Letters, 06/2000, Vol.2(11), pp.1501-1504 [Peer Reviewed Journal]

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9
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Effects of temperature and concentration in some ring closing metathesis reactions

Yamamoto, Kana ; Biswas, Kaustav ; Gaul, Christoph ; Danishefsky, Samuel J

Tetrahedron Letters, 2003, Vol.44(16), pp.3297-3299 [Peer Reviewed Journal]

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Effects of temperature and concentration in some ring closing metathesis reactions
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Effects of temperature and concentration in some ring closing metathesis reactions

Yamamoto, Kana ; Biswas, Kaustav ; Gaul, Christoph ; Danishefsky, Samuel J.

Tetrahedron Letters, 4/2003, Vol.44(16), pp.3297-3299 [Peer Reviewed Journal]

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11
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Discovery of potent cell migration inhibitors through total synthesis: lessons from structure-activity studies of (+)-migrastatin

Njardarson, Jón T ; Gaul, Christoph ; Shan, Dandan ; Huang, Xin-Yun ; Danishefsky, Samuel J

Journal of the American Chemical Society, 04 February 2004, Vol.126(4), pp.1038-40 [Peer Reviewed Journal]

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12
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Design, synthesis, and evaluation of matrix metalloprotease inhibitors bearing cyclopropane-derived peptidomimetics as P1' and P2' replacements

Reichelt, Andreas ; Gaul, Christoph ; Frey, Robin R ; Kennedy, April ; Martin, Stephen F

The Journal of organic chemistry, 14 June 2002, Vol.67(12), pp.4062-75 [Peer Reviewed Journal]

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13
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The migrastatin family: discovery of potent cell migration inhibitors by chemical synthesis

Gaul, Christoph ; Njardarson, Jón T ; Shan, Dandan ; Dorn, David C ; Wu, Kai-Da ; Tong, William P ; Huang, Xin-Yun ; Moore, Malcolm A S ; Danishefsky, Samuel J

Journal of the American Chemical Society, 15 September 2004, Vol.126(36), pp.11326-37 [Peer Reviewed Journal]

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14
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Computational, ReactIR‐, and NMR‐Spectroscopic Investigations on the Chiral Formyl Anion Equivalent N ‐( α ‐Lithiomethylthiomethyl)‐4‐isopropyl‐5,5‐diphenyloxazolidin‐2‐one and Related Compounds

Gaul, Christoph ; Arvidsson, Per I. ; Bauer, Walter ; Gawley, Robert E. ; Seebach, Dieter

Chemistry – A European Journal, 01 October 2001, Vol.7(19), pp.4117-4125 [Peer Reviewed Journal]

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15
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Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket

Scheufler, Clemens ; Möbitz, Henrik ; Gaul, Christoph ; Ragot, Christian ; Be, Céline ; Fernández, César ; Beyer, Kim S ; Tiedt, Ralph ; Stauffer, Frédéric

ACS medicinal chemistry letters, 11 August 2016, Vol.7(8), pp.730-4 [Peer Reviewed Journal]

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16
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Applications of the Chiral Auxiliaries DIOZ and TRIOZ for Conjugate Additions and Comparison with Other Auxiliaries

Sprecher, Hanspeter ; Pletscher, Stefan ; Möri, Manuel ; Marti, Roger ; Gaul, Christoph ; Patora‐Komisarska, Krystyna ; Otchertianova, Ekatarina ; Beck, Albert K. ; Seebach, Dieter

Helvetica Chimica Acta, January 2010, Vol.93(1), pp.90-110 [Peer Reviewed Journal]

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17
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Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach

Möbitz, Henrik ; Machauer, Rainer ; Holzer, Philipp ; Vaupel, Andrea ; Stauffer, Frédéric ; Ragot, Christian ; Caravatti, Giorgio ; Scheufler, Clemens ; Fernandez, Cesar ; Hommel, Ulrich ; Tiedt, Ralph ; Beyer, Kim S ; Chen, Chao ; Zhu, Hugh ; Gaul, Christoph

ACS medicinal chemistry letters, 09 March 2017, Vol.8(3), pp.338-343 [Peer Reviewed Journal]

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18
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2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes

van Eis, Maurice J ; Evenou, Jean-Pierre ; Floersheim, Philipp ; Gaul, Christoph ; Cowan-Jacob, Sandra W ; Monovich, Lauren ; Rummel, Gabriele ; Schuler, Walter ; Stark, Wilhelm ; Strauss, Andre ; Matt, Anette Von ; Vangrevelinghe, Eric ; Wagner, Juergen ; Soldermann, Nicolas

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(24), pp.7367-7372 [Peer Reviewed Journal]

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19
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Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach

Chen, Chao ; Zhu, Hugh ; Stauffer, Frédéric ; Caravatti, Giorgio ; Vollmer, Susanne ; Machauer, Rainer ; Holzer, Philipp ; Möbitz, Henrik ; Scheufler, Clemens ; Klumpp, Martin ; Tiedt, Ralph ; Beyer, Kim S ; Calkins, Keith ; Guthy, Daniel ; Kiffe, Michael ; Zhang, Jeff ; Gaul, Christoph

ACS medicinal chemistry letters, 11 August 2016, Vol.7(8), pp.735-40 [Peer Reviewed Journal]

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20
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Metallations and Reactions with Electrophiles of 4‐Isopropyl‐5,5‐diphenyloxazolidin‐2‐one (DIOZ) with N ‐Allyl and N ‐Propargyl Substituents: Chiral Homoenolate Reagents

Gaul, Christoph ; Seebach, Dieter

Helvetica Chimica Acta, April 2002, Vol.85(4), pp.963-978 [Peer Reviewed Journal]

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21
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Identification of orally available naphthyridine protein kinase D inhibitors

Meredith, Erik L ; Ardayfio, Ophelia ; Beattie, Kimberly ; Dobler, Markus R ; Enyedy, Istvan ; Gaul, Christoph ; Hosagrahara, Vinayak ; Jewell, Charles ; Koch, Keith ; Lee, Wendy ; Lehmann, Hansjoerg ; Mckinsey, Timothy A ; Miranda, Karl ; Pagratis, Nikos ; Pancost, Margaret ; Patnaik, Anup ; Phan, Dillon ; Plato, Craig ; Qian, Ming ; Rajaraman, Vasumathy ; Rao, Chang ; Rozhitskaya, Olga ; Ruppen, Thomas ; Shi, Jie ; Siska, Sarah J ; Springer, Clayton ; Van Eis, Maurice ; Vega, Richard B ; Von Matt, Anette ; Yang, Lihua ; Yoon, Taeyoung ; Zhang, Ji-Hu ; Zhu, Na ; Monovich, Lauren G

Journal of medicinal chemistry, 12 August 2010, Vol.53(15), pp.5400-21 [Peer Reviewed Journal]

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22
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Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors

Pissot-Soldermann, Carole ; Gerspacher, Marc ; Furet, Pascal ; Gaul, Christoph ; Holzer, Philipp ; Mccarthy, Clive ; Radimerski, Thomas ; Regnier, Catherine H ; Baffert, Fabienne ; Drueckes, Peter ; Tavares, Gisele A ; Vangrevelinghe, Eric ; Blasco, Francesca ; Ottaviani, Giorgio ; Ossola, Flavio ; Scesa, Julien ; Reetz, Janitha

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(8), pp.2609-2613 [Peer Reviewed Journal]

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23
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Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition

Weigert, Oliver ; Bird, Liat ; Kopp, Nadja ; Van Bodegom, Diederik ; Marubayashi, Sachie ; Christie, Amanda L. ; Paranal, Ronald M. ; Gaul, Christoph ; Vangrevelinghe, Eric ; Romanet, Vincent ; Murakami, Masato ; Tiedt, Ralph ; Ebel, Nicolas ; Evrot, Emeline ; De Pover, Alain ; Régnier, Catherine H. ; Erdmann, Dirk ; Hofmann, Francesco ; Levine, Ross L. ; Baffert, Fabienne ; Radimerski, Thomas ; Lane, Andrew Alan ; Chapuy, Bjoern ; Toms, Angela Vivian ; Mckeown, Michael Robert ; Bradner, James Elliott ; Yoda, Akinori ; Eck, Michael Joseph ; Sallan, Stephen Earl ; Kung, Andrew ; Weinstock, David Marc

Weigert, Oliver, Andrew A. Lane, Liat Bird, Nadja Kopp, Bjoern Chapuy, Diederik van Bodegom, Angela V. Toms, et al. 2012. Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition. The Journal of Experimental Medicine 209(2): 259-273. [Peer Reviewed Journal]

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24
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Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent

Andraos, Rita ; Qian, Zhiyan ; Bonenfant, Débora ; Rubert, Joëlle ; Vangrevelinghe, Eric ; Scheufler, Clemens ; Marque, Fanny ; Régnier, Catherine H ; De Pover, Alain ; Ryckelynck, Hugues ; Bhagwat, Neha ; Koppikar, Priya ; Goel, Aviva ; Wyder, Lorenza ; Tavares, Gisele ; Baffert, Fabienne ; Pissot-Soldermann, Carole ; Manley, Paul W ; Gaul, Christoph ; Voshol, Hans ; Levine, Ross L ; Sellers, William R ; Hofmann, Francesco ; Radimerski, Thomas

Cancer discovery, June 2012, Vol.2(6), pp.512-523

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25
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2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors

Gerspacher, Marc ; Furet, Pascal ; Pissot-Soldermann, Carole ; Gaul, Christoph ; Holzer, Philipp ; Vangrevelinghe, Eric ; Lang, Marc ; Erdmann, Dirk ; Radimerski, Thomas ; Regnier, Catherine H ; Chene, Patrick ; Pover, Alain De ; Hofmann, Francesco ; Baffert, Fabienne ; Buhl, Thomas ; Aichholz, Reiner ; Blasco, Francesca ; Endres, Ralf ; Trappe, Jörg ; Drueckes, Peter

Bioorganic & Medicinal Chemistry Letters, 2010, Vol.20(5), pp.1724-1727 [Peer Reviewed Journal]

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26
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Crystal Structures – A Manifesto for the Superiority of the Valine‐Derived 5,5‐Diphenyloxazolidinone as an Auxiliary in Enantioselective Organic Synthesis

Gaul, Christoph ; Schweizer, Bernd W. ; Seiler, Paul ; Seebach, Dieter

Helvetica Chimica Acta, June 2002, Vol.85(6), pp.1546-1566 [Peer Reviewed Journal]

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27
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CCDC 1546562: Experimental Crystal Structure Determination

Fairhurst, Robin A. ; Knoepfel, Thomas ; Leblanc, Catherine ; Buschmann, Nicole ; Gaul, Christoph ; Blank, Jutta ; Galuba, Inga ; Trappe, Jörg ; Zou, Chao ; Voshol, Johannes ; Genick, Christine ; Brunet-Lefeuvre, Peggy ; Bitsch, Francis ; Graus-Porta, Diana ; Furet, Pascal

2017

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28
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New applications of the chiral auxiliary 4-isopropyl-5,5-diphenyloxazolidinone in enantioselective transformations

Gaul, Christoph Vasella, Andrea Thaddäus; Seebach, Dieter

2002

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