First Direct Trifluoromethoxylation of Aryl Halides Achieved by the Team of Professor Tang Pingping at Nankai University

First Direct Trifluoromethoxylation of Aryl Halides Achieved by the Team of Professor Tang Pingping at Nankai University

The trifluoromethoxy group (-OCF3) is a highly valuable functional group in the design of pharmaceutical and pesticide molecules—its unique stereostructure (perpendicular to the aromatic ring plane) can significantly enhance the binding ability of molecules to biological targets. Additionally, its strong electron-withdrawing nature and high lipophilicity can improve the metabolic stability and cell membrane permeability of … Read more

Multi-Kg Production of 3-Fluoro-6-methoxyquinoline

Multi-Kg Production of 3-Fluoro-6-methoxyquinoline

Org. Process Res. Dev. 2022, 26, 347. DOI: 10.1021/acs.oprd.1c00414 Route A ◆During the aqueous quench, a certain degree of back-hydrolysis to 2 occurred, which contaminated the initial crude product. The problem was solved by performing the chlorination with diphenylphosphoryl chloride (1.5 equiv) in DMF (5.5 vol). ◆For the Hofmann rearrangement of 11, the conditions reported … Read more