Sodium Sulfate → HCID 68566704, compound

Participants

Reaction Steps

To a solution of (3R,4S)-4-amino-3-(trifluoromethyl)piperidine-1-carboxylic acid tert-butyl ester (2d) (1 equiv.) in acetonitrile is added Na2SO4 and 3-oxo-3,4-dihydro-2H-benzo[1,4]thiazine-6-carboxaldehyde (in) (1 equiv.). After 12 hr at RT, the reaction is filtered through a sintered-glass funnel and the filtrate is concentrated under vacuum. The remaining residue is dissolved in EtOH and NaBH4 (1 equiv.) is added. After 12 h, the reaction is concentrated and the residue is dissolved in 1 N HCl. The solution is neutralized with 6 N NaOH and extracted with EtOAc. The organic fraction is dried over Na2SO4 and concentrated under vacuum. The crude product is purified by flash chromatography on silica gel to afford the title compound.

Provenance & Evidence