Initial Route Scouting and Final Process Development for the Multi-Kg Production of 3-Fluoro-6-methoxyquinoline from p-Anisidine and 2-Fluoromalonic Acid

Author:

Schäfer Gabriel1ORCID,Fleischer Tony1,Blumer Nicole1,Udry Megan1,Reber Stefan1,Stansfield Ian2,Liu Yuanhua2,Li Yan2,Li Pixu2

Affiliation:

1. Chemistry Process R&D, Idorsia Pharmaceuticals Ltd., Hegenheimermattweg 91, CH-4123 Allschwil, Switzerland

2. Chiral Quest (Suzhou) Co., Limited, 268 ChangAn Road, Wujiang, Suzhou, Jiangsu 215200, China

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Reference14 articles.

1. Hubschwerlen, C.; Rueedi, G.; Surivet, J.P.; Zumbrunn, C. (Actelion Pharmaceuticals Ltd. Switzerland). 4-(1-amino-ethyl)-cyclohexylamine derivatives. U.S. Patent 20,100,029,623 A1, 2010.

2. Über aromatische Fluorverbindungen, I.: Ein neues Verfahren zu ihrer Darstellung

3. El-Ahmad, Y.; Leconte, J.P.; Malpart, J.; Mignani, S.; Mutti, S.; Tabart, M. (Aventis Pharmeceuticals Inc. USA). Novel Process for preparing 3-fluoroquinolines. WO 2005049575 A1, 2005.

4. A One-Pot Diazotation–Fluorodediazoniation Reaction and Fluorine Gas for the Production of Fluoronaphthyridines

5. Where Does the Fluorine Come From? A Review on the Challenges Associated with the Synthesis of Organofluorine Compounds

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