反应详情

A solution of acetyl chloride (552 mg, 500 μL, 7.03 mmol, Eq: 115) in MeOH (2 mL) was added to a vial containing ((S)-1-{(S)-1-[(S)-1-(2-chloro-6-fluoro-phenylcarbamoyl)-3,4-dihydro-1H-isoquinoline-2-carbonyl]-2-methyl-propylcarbamoyl}-ethyl)-methyl-carbamic acid tert-butyl ester (36 mg, 61.1 μmol, Eq: 1.00). The mixture was stirred at RT for 1 h. The solvent was evaporated and the resulting solid was dissolved in MeCN (3 mL) and water (1 mL) which was lyophilized to give (S)-2-[(S)-3-methyl-2-((S)-2-methylamino-propionylamino)-butyryl]-1,2,3,4-tetrahydro-isoquinoline-1-carboxylic acid (2-chloro-6-fluoro-phenyl)-amide hydrochloride (30 mg) as a white powder, m/z=489 (M+H).

1. customThe solvent was evaporated
2. dissolutionthe resulting solid was dissolved in MeCN (3 mL)