Hydrochloric Acid → HCID 90015738, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of (R)-ethyl 1-(2-(5-bromo-2-fluorophenyl)-2-(2,4-dimethoxybenzylamino)propylthio)cyclobutanecarboxylate (2 g, 3.7 mmol, Eq: 1.00) in ethanol (50 ml) was added 3 N NaOH (2.47 ml, 7.4 mmol, Eq: 2.0). The reaction solution was stirred at 70° C. for 2 hours. 1 N HCl (7.4 ml, 7.4 mmol, Eq: 2.0) was added to the reaction mixture at 23° C. (pH=5-6). After evaporation the residue was triturated with dichloromethane/methanol 9:1 and solid Na2SO4 was added. The solid was filtered off and the filtrate was evaporated to dryness to give the crude (R)-1-(2-(5-bromo-2-fluorophenyl)-2-(2,4-dimethoxybenzylamino)propylthio)cyclobutanecarboxylic acid (1.8 g, 3.51 mmol, 94.9% yield) as a white foam, which was used without further purification. MS (ISP): m/z=512.4 [M+H]+ and 514.4 [M+2+H]+.

Provenance & Evidence