Triphenylphosphine → ethyl 5-(4-((4-(5-amino-1-(tert-butoxycarbonyl)-4-cyano-1H-pyrazol-3-yl)phenoxy)methyl)phenyl)-2-(8-(benzo[d]thiazol-2-yl((2-(trimethylsilyl)ethoxy)methyl)carbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)thiazole-4-carboxylate

Participants

Reaction Conditions

Reaction Steps

A mixture of compound 34D (0.14 g, 0.2 mmol), PPh3 (0.079 g, 0.3 mmol), and compound 31F (0.066 g, 0.022 mmol) was dissolved in THF (3 mL). The solution was cooled to 0° C. To this solution was added DBAD. The reaction mixture was stirred at rt for 2 hours. The solvent was removed, and the residue was purified by flash column chromatography on silica gel eluting with 2:1/hexanes:EtOAc to afford 0.13 g of the title compound as a mixture of two inseparable isomers. MS (ESI(+)): m/z 982 (M+NH4—H2O).

Provenance & Evidence