Acetic Acid → (2S)-2-(5-(N-2-picolylaminomethyl)thiophene-2-carbonylamino)-5-(5,6,7,8-tetrahydroquinolin-8-ylamino)valeric Acid

Participants

Reaction Steps

The compound obtained in Example 14-4 (18.2 mg) was dissolved in methanol (0.6 ml), and acetic acid (0.06 ml), 5,6,7,8-tetrahydroquinolin-8-one (16 mg), and sodium cyanoborohydride (7 mg) were added. After 3 days, the reaction solution was concentrated. The residue was purified by silica gel column chromatography (1 g, chloroform/methanol=5/1). 1 mol/l hydrochloric acid was added to the resulting colorless syrup, and the mixture was concentrated and dried under reduced pressure to obtain ahydrochloride of the title compound (6.7 mg) as a white solid.

Provenance & Evidence