Thiomorpholine, 4-(2,6-difluoro-4-nitrophenyl)-, 1,1-dioxide → 4-(4-Amino-2,6-difluorophenyl)-1lambda~6~,4-thiazinane-1,1-dione

Participants

Reaction Conditions

Reaction Steps

To an autoclave is added the product of example 2 (7.0 kg, 24 moles, 1.0 eq). Raney Nickel (1.4 kg) is activated and suspended in 4 L of THF. The slurry is added to the autoclave followed by additional THF (66 L). The mixture is heated at 40° C. and under 40 psi H2 till completion. The mixture is filtered and the filtrate is directly used in the next step. A small portion of the filtrate is concentrated and recrystallized in isopropanol to give the title compound.

Provenance & Evidence