Triethylamine → methyl N-({2-amino-5-[(1-bromo-2-methylindolizin-3-yl)carbonyl]phenyl}carbonyl)glycinate

Participants

Reaction Conditions

Reaction Steps

Triethylamine (7.34 mL; 52.3 mmol) and PyBOP (9.97 g; 19.2 mmol) are added to a solution of 2-amino-5-[(1-bromo-2-methylindolizin-3-yl)carbonyl]benzoic acid (6.5 g; 17.4 mmol) in 58 mL of NMP at 0° C. under nitrogen. After 30 min of stirring at 0° C., glycine methyl ester hydrochloride (2.4 g; 19.2 mmol) is added. After 1 h of stirring at ambient temperature, the reaction medium is run into a saturated aqueous solution of sodium hydrogen carbonate. The yellow precipitate formed is filtered off and dried under vacuum to give 6.45 g (83%) of a yellow powder.

Provenance & Evidence