5,6-diethoxy-7-fluoro-3H-isoindol-1-ylamine → Atopaxar Hydrobromide

Participants

Reaction Conditions

Reaction Steps

2-Bromo-1-(3-tert-butyl-4-methoxy-5-morpholinophenyl)ethanone (550 g, 1.485 mol) was dissolved in tetrahydrofuran (3 L) and subjected to clarifying filtration. A solution of 5,6-diethoxy-7-fluoro-3H-isoindol-1-ylamine (300 g, 1.254 mol) in tetrahydrofuran (4.5 L) was added dropwise to the above solution in 3 portions (100 g/1.5 L×3 times) while stirring at the ambient temperature of 6° C. After completion of the dripping, crystals were deposited. After stirring for 18 hours, the deposited crystals were collected by filtration and washed with ice-cooled tetrahydrofuran (1.2 L) to give 696.5 g of the captioned compound as wet crystals.

Provenance & Evidence