Trifluoroacetic acid → 2-Amino-3-[7-(6,7-difluoroquinolin-2-ylmethoxy)-11-methyl-10,11-dihydro-5h-benzo[e]pyrido[2,3-b]azepin-5-ylsulfanyl]-propionic acid ethyl ester

Participants

Reaction Conditions

Reaction Steps

A mixture of 6.6 g (15.7 mmol) of the product from Example 21, step 5, 6.0 g (32.3 mmol) of L-cystein ethyl ester hydrochloride and 136 ml of trifluoroacetic acid in 198 ml of dichloromethane is stirred at 45° C. for 16 hr. The solvent is evaporated and the residue partitioned between sat. NaHCO3 and chloroform. The organic layer is washed with water, dried and concentrated, giving an oil, which solidifies with the aid of diisopropyl ether/petroleum ether. Yield 7.9 g (91%).

Provenance & Evidence