2-(Thiophen-2-yl)benzoic acid → (1R,6S)-8-(3,6-Dimethylpyrazin-2-yl)-3-{[2-(2H-1,2,3-triazol-2-yl)phenyl]carbonyl}-3,8-diazabicyclo[4.2.0]octane

Participants

Reaction Steps

The title compound was prepared in a manner analogous to Example 1, substituting (1R,6S)-8-(3,6-dimethyl-pyrazin-2-yl)-3,8-diaza-bicyclo[4.2.0]octane (Intermediate 10) for (1R,6S)8-(4,6-dimethyl-pyrimidin-2-yl)-3,8-diaza-bicyclo[4.2.0]octane and 2-[1,2,3]triazol-2-yl-benzoic acid (Intermediate 14) for 2-thiophen-2-yl-benzoic acid and DCM in place of DMF. DCM was used in place of DMF. MS (ESI) mass calcd. For O21H23N7O, 389.46; m/z found 390.1 [M+H]+. 1H NMR (CDCl3): 8.03-7.91 (m, 1H), 7.81-7.64 (m, 2H), 7.54-7.20 (m, 3H), 6.99-6.87 (m, 1H), 4.87-3.93 (m, 4H), 3.78-3.48 (m, 2H), 3.29-2.75 (m, 2H), 2.39-2.29 (m, 4H), 2.06-2.02 (m, 4H).

Provenance & Evidence