1-Hydroxybenzotriazole → HCID 178522664, compound

Participants

Reaction Steps

A mixture of 66.7 mg product from Step F above, 71.9 mg EDC, 30.4 mg HOBt and 23.2 mg aminotetrazole monohydrate was dissolved in 1 mL DMF. DIEA (92 μL) was added immediately and the resulting solution was stirred at room temperature for 17 hours. The reaction mixture was diluted with a mixture of DMSO, MeCN, and water and purified on preparative HPLC using 65˜80% MeCN gradient over 10 minutes at 8.0 mL per minute with 0.1% TFA. The title compound was obtained as a white solid following lyophilization. 1H NMR (DMSO-d6, 500 MHz) δ 8.045 (d, J=8.2 Hz, 2H), 7.50˜7.54 (m, 4H), 7.41 (d, J=8.2 Hz, 2H), 7.33 (s, 1H), 4.06 (s, 2H), 2.64 (tt, J=3.0 & 12.2 Hz, 1H), 1.62˜1.72 (m, 4H), 1.48˜1.48 (m, 3H), 1.05˜1.15 (m, 3H). LC-MS: 1.97 min. (M+H=512.2).

Provenance & Evidence