p-Toluenesulfonic acid monohydrate → HCID 86644640, compound

Participants

Reaction Steps

To a mixture of tert-butyl rel-(1R,2S)-2-[(tert-butoxycarbonyl)amino]cyclopropanecarboxylate (0.54 g) and diethyl ether (4.0 ml) was added a solution of p-toluene sulfonic acid monohydrate (0.40 g) in diethyl ether (16 ml) at room temperature, followed by stirring at room temperature for 5 hours. The reaction mixture was concentrated under reduced pressure to obtain tert-butyl rel-(1R,2S)-2-aminocyclopentanecarboxylate p-toluene sulfonate (0.68 g). Tert-butyl rel-(1R,2S)-2-({N5-[(benzyloxy)carbonyl]-N2-[(1-methyl-1H-indol-2-yl)carbonyl]-L-ornithyl}amino)cyclopropanecarboxylate (0.20 g) was obtained by using tert-butyl rel-(1R,2S)-2-aminocyclopropanecarboxylate p-toluene sulfonate (0.64 g) in the same method as for Production Process A1.

Provenance & Evidence