反应详情

40 mg of N-[(1S,2R)-1-(3,5-difluorobenzyl)-2-hydroxy-3-({1-[3-(trifluoromethyl)phenyl]cyclopropyl}amino)propyl]-1-oxo-2-(1-propylbutyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxamide are dissolved in 10 cm3 of ethyl ether at a temperature close to 20° C. 3 cm3 of a 1M hydrochloric acid solution in ether are added while stirring under argon. The reaction mixture precipitates. The precipitate is filtered through sintered glass, washed with 3 lots of 5 cm3 of ethyl ether then dried in a desiccator under vacuum at 35° C. for 2 h. 129 mg of N-[(1S,2R)-1-(3,5-difluorobenzyl)-2-hydroxy-3-({1-[3-(trifluoromethyl)phenyl]cyclopropyl}amino)propyl]-1-oxo-2-(1-propylbutyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxamide hydrochloride (1:1) are obtained in the form of a white solid.

1. customclose to 20° C
2. customThe reaction mixture precipitates
3. filtrationThe precipitate is filtered through sintered glass
4. washwashed with 3 lots of 5 cm3 of ethyl ether
5. customthen dried in a desiccator under vacuum at 35° C. for 2 h