反应详情

750 mg (1.44 mmol) of tert-butyl 1-(3-{[(4-chlorophenyl)(2,2-difluorocyclopentyl)acetyl]amino}-4-fluorobenzyl)cyclopropanecarboxylate (as racemic diastereomer mixture) were dissolved in 1.6 ml of dichloromethane, and 5.5 ml of TFA were added at RT. The mixture was stirred at RT for 2 h and then concentrated under reduced pressure. The residue was dried under high vacuum and then triturated with acetonitrile. The precipitated solid was filtered off. The filtrate was concentrated, the residue obtained was once more triturated with acetonitrile and a further batch of solid was isolated. This procedure was repeated once more, and all solid batches were then combined. This gave a total of 553 mg (82.6% of theory) of the title compound as a mixture of four isomers.

1. concentrationconcentrated under reduced pressure
2. customThe residue was dried under high vacuum
3. customtriturated with acetonitrile
4. filtrationThe precipitated solid was filtered off
5. concentrationThe filtrate was concentrated
6. customthe residue obtained
7. customwas once more triturated with acetonitrile
8. customa further batch of solid was isolated