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