Pyrazole → HCID 57937391, compound

Participants

Reaction Steps

Following the same procedure in Example 1, Step A, using 2-tert-butyl-1-[(4,4-difluorocyclohexyl)methyl]-1H-benzimidazole-5-sulfonyl chloride (202 mg, 0.5 mmol) and pyrazol (186 mg, 2.7 mmol) in MeCN (6 mL). The crude product was purified by MPLC using Hex/EtOAc (1:1) on silica gel to give 164 mg (75%) of a white solid as the title compound. 1H NMR (400 MHz, CHLOROFORM-D) δ 1.43-1.54 (m, 1 H), 1.56 (s, 9 H), 1.59-1.80 (m, 4 H), 2.01-2.22 (m, 3 H), 2.49-2.79 (m, 1 H), 4.24 (d, J=7.42 Hz, 2 H), 6.38 (dd, J=2.73, 1.56 Hz, 1 H), 7.43 (d, J=8.59 Hz, 1 H), 7.70 (d, J=0.98 Hz, 1 H), 7.96 (dd, J=8.69, 1.66 Hz, 1 H), 8.15 (d, J=2.73 Hz, 1 H), 8.40 (d, J=1.76 Hz, 1 H); MS (ESI) (M+H)+=437.3; Anal. Calcd for C21H26F2N4O2S+0.2H2O (440.13): C, 57.31; H, 6.05; N, 12.73. Found: C, 57.23; H, 6.05; N, 12.83.

Provenance & Evidence