Ammonia → HCID 58789219, compound

Participants

Reaction Conditions

Reaction Steps

To a steel bomb charged with N,N-dibenzyl-1-chloro-7-fluoroisoquinolin-6-amine (3.953 g, 10.49 mmol, see WO 2007/002313 for preparation) was added 15 mL of 7N NH3 in ethylene glycol (prepared by condensing ammonia in ethylene glycol) and the reaction sealed and heated at 165° C. overnight (20 h). The reaction mixture was poured into sat. NaHCO3 (200 mL) and extracted with DCM (3×200 mL). The combined organics were washed with brine (150 mL) and dried (Na2SO4), filtered and concentrated to leave Intermediate 4A (3.71 g, 99% yield) as a yellow solid. MS (ESI) m/z: 358.1 [M+1]+.

Provenance & Evidence