Trifluoroacetic acid → HCID 68834206, compound

Participants

Reaction Steps

Deprotection of N1-BOC-(1S,3R)-3-(2H-1,2,3-triazol-2-ylmethyl)cyclopentan-1-amine (500 mg, 1.87 mmol) using TFA (3 ml) in dry dichloromethane (3 ml) as described in Example 1, Step 2 gave 528 mg of the amine as its TFA salt, which was used as such for the coupling reaction. Step 3: Coupling reaction of Step 2 intermediate (528 mg, 1.87 mmol) with Intermediate 17 (162 mg, 0.94 mmol) in the presence of potassium carbonate (780 g, 5.63 mmol) and NaI (141 mg, 0.94 mmol) in THF (30 ml) as described in Example 1, Step 3 gave 90 mg of the product as a white solid; IR (KBr) 3437, 2955, 2236, 1656, 1420 cm−1; 1H NMR (CDCl3, 300 MHz) δ 1.16–1.25 (m, 1H), 1.46–1.62 (m, 2H), 1.70–1.87 (m, 3H), 1.95–2.34 (m, 5H), 2.54–2.65 (m, 1H), 3.09–3.18 (m, 1H), 3.36–3.62 (m, 4H), 4.43 (d, J=7.2 Hz, 2H), 4.76–4.78 (m, 1H), 7.58 (s, 2H).

Provenance & Evidence