Cyclopropylamine → (2S)-1-[(3R)-3-amino-4-phenylbutanoyl]-N-({5-chloro-2-[(cyclopropylcarbamoyl)methoxy]phenyl}methyl)pyrrolidine-2-carboxamide

Participants

Reaction Steps

A solution of 46 mg (0.08 mmol) of the tert butyl carbamate of {2-[({1-[(3R)-3-amino-4-phenylbutanoyl]-L-prolyl}amino)methyl]-4-chlorophenoxyacetic acid and 0.0055 mL (0.096 mmol) of cyclopropylamine in DMF were coupled and deprotected as described for Example 1, Step C and D to give 25 mg of the title compound. 1H NMR (400 MHz, CD3OD) δ 7.32–7.10 (m, 7H), 6.95 (d, 0.2H, J=8 Hz), 6.85 (d, 0.8H, J=8 Hz), 4.55–4.22 (m, 5H), 3.61–3.35 (m, 3H), 2.82–2.50 (m, 4H), 2.38–2.10 (m, 2H), 2.07–1.80 (m, 3H), 0.75–0.58 (m, 4H).

Provenance & Evidence