HCID 58717298, compound → di-tert-butyl (6-{[(4-bromo-1-trityl-1H-imidazol-2-yl)(3-chloro-5-ethyl-2-fluorophenyl)methyl]amino}isoquinolin-1-yl)imidodicarbonate

Participants

Reaction Steps

According to the procedure for the preparation of Intermediate 206.4, Intermediate 221.2 (309 mg, 0.537 mmol) was converted to the chloro intermediate, then displaced with di-tert-butyl (6-aminoisoquinolin-1-yl)imidodicarbonate (rt for 15 h, 40° C. for 9 h, 50° C. for 6 h) to afford after flash chromatography (O to 50% EtOAc/hexanes gradient) 400 mg of Iintermediate 221.3 as a pale yellow solid. LCMS (50 to 100% B, 4 min gradient, A=95% H2O/5% CH3CN/0.1% TFA, B=5% H2O/95% CH3CN/0.1% TFA) RT=5.43 min, 918.76 (M+H)+.

Provenance & Evidence