Scalable Synthesis of Trifluoromethylated Imidazo-Fused N‑Heterocycles Using TFAA and Trifluoroacetamide as CF3‑Reagents von Schäfer, Gabriel, Ahmetovic, Muhamed, Abele, Stefan

Volltext

Development of a 2nd Generation Process for 3‐Ethyl‐4‐Hydroxy‐5‐Methylbenzonitrile – A Key Building Block of S1P1 Receptor Modulator Cenerimod – through a Non‐Classical Nitrile For... von Schäfer, Gabriel, Fleischer, Tony

Volltext

Development of a Scalable, Racemic First-Generation Route for CXCR7 Antagonist ACT-1004-1239 via cis-to-trans Epimerization and Subsequent Separation of Enantiomers von Schäfer, Gabriel, Fleischer, Tony, Ahmetovic, Muhamed, Guerry, Philippe, Abele, Stefan

Volltext

Sandmeyer Chlorosulfonylation of (Hetero)Aromatic Amines Using DABSO as an SO2 Surrogate von Pincekova, Lucia, Merot, Aurélien, Schäfer, Gabriel, Willis, Michael C.

Volltext

Discovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239 von Richard-Bildstein, Sylvia, Aissaoui, Hamed, Pothier, Julien, Schäfer, Gabriel, Gnerre, Carmela, Lindenberg, Eleanor, Lehembre, François, Pouzol, Laetitia, Guerry, Philippe

Volltext

Development of a Scalable Route toward an Alkylated 1,2,4-Triazol, a Key Starting Material for CXCR3 Antagonist ACT-777991 von Davenport, Raffael, Prud’homme, Alice, Masse, Florence, Schäfer, Gabriel

Volltext

Suzuki–Miyaura Coupling of Aryl Nosylates with Diethanolamine Boronates von Kohler, Philipp, Perrin, Timothé, Schäfer, Gabriel

Volltext

Development of a Scalable, Stereoselective Second-Generation Route for CXCR7 Antagonist ACT-1004-1239 via Chiral Enamine Reduction and a Novel Telescoped Sequence of Transesterific... von Schäfer, Gabriel, Fleischer, Tony, Merot, Aurélien, Erhardt, Michael, Mathys, Boris

Volltext

Scalable, Chromatography‐Free Synthesis of 2‐(3‐Bromophenyl)‐2H‐1,2,3‐triazole through N−N Bond Forming Cyclization von Kohler, Philipp, Schindelholz, Ivan, Schäfer, Gabriel

Volltext

Scalable Synthesis of C5aR1 Antagonist ACT-1014-6470 via N 7‑Selective Reductive Amination of an Unprotected Pyrazole Starting Material and Intramolecular Urea Formation with 1,1′-... von Reber, Stefan, Blumer, Nicole, Leuenberger, Daniel, Fleischer, Tony, Renneberg, Dorte, Abele, Stefan, Schäfer, Gabriel

Volltext

Facile Synthesis of Sterically Hindered and Electron-Deficient Secondary Amides from Isocyanates von Schäfer, Gabriel, Matthey, Coraline, Bode, Jeffrey W.

Volltext

Development of a Scalable Electrophilic Amination Protocol for the Multi-kg Production of 5‑Methyl-2-pyridinesulfonamide: A Regulatory Starting Material of Endothelin Receptor Anta... von Schäfer, Gabriel, Fleischer, Tony, Kastner, Matthias, Karge, Reinhard, Huang, Qi, Wu, Bruce Libang, Tang, Jun, Aiglstorfer, Iris

Volltext

Synthesis of (1 R )‐1‐(4‐Bromophenyl)‐2,2,2‐trifluoroethan‐1‐amine Hydrochloride through Diastereoselective Trifluoromethylation of a Chiral Sulfinimine von Wolleb, Helene, Bonina, Francesco, Udry, Megan, Reber, Stefan, Blumer, Nicole, Leuenberger, Daniel, Schäfer, Gabriel

Volltext

Large-Scale Synthesis of LPA1-Receptor Antagonist ACT-1016-0707 von Davenport, Raffael, Masse, Florence, Prud’homme, Alice, Bürki, Cédric, Doerrwaechter, Patric, Künzli, Marco, D’Aiuto, Fabio, Bolli, Martin H., Schäfer, Gabriel

Volltext

Synthesis of Methyl 3‑Hydroxyisoxazole-5-Carboxylate Via Bromination of Dimethyl Fumarate under Photoflow Conditions and Its Safe Homologation into 3‑(3-Methoxyisoxazol-5-yl) Propa... von Bürki, Cédric, Künzli, Marco, Dörrwächter, Patric, Wallquist-Franke, Patrick, Wang, Larry Y., Zhang, Feng, Schäfer, Gabriel

Volltext

Discovery of the Clinical Candidate IDOR-1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases von Meyer, Emmanuel A., Croxford, Andrew L., Gnerre, Carmela, Kulig, Paulina, Murphy, Mark J., Jacob, Elise M., Schäfer, Gabriel, Richard-Bildstein, Sylvia, Aissaoui, Hamed, Bouis, Patrick, Ertel, Eric A., de Kanter, Ruben, Keller, Marcel P., Lüthi, Urs, Caroff, Eva

Volltext

Development of a Scalable Route for a Key Benzothiazole Building Block via a Pd-Catalyzed Migita Coupling with a Nonsmelly Thiol Surrogate von Schäfer, Gabriel, Merot, Aurélien, Fleischer, Tony

Volltext

Friedel-Crafts Benzylation of Activated and Deactivated Arenes von Schäfer, Gabriel, Bode, Jeffrey W.

Volltext

Synthesis of Sterically Hindered N‑Acylated Amino Acids from N‑Carboxyanhydrides von Schäfer, Gabriel, Bode, Jeffrey W

Volltext

Development of a Scalable Route for a Key Thiadiazole Building Block via Sequential Sandmeyer Bromination and Room-Temperature Suzuki–Miyaura Coupling von Schäfer, Gabriel, Fleischer, Tony, Ahmetovic, Muhamed, Abele, Stefan

Volltext