Azetidine → HCID 57937367, 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 (122 mg, 0.3 mmol), azetidine (41 uL, 34 mg, 0.6 mmol) and DMAP (73 mg, 0.6 mmol) in MeCN (5 mL). The crude product was purified by MPLC using Hex/EtOAc (1:1) on silica gel to give 88 mg (69%) of a white solid as the title compound. 1H NMR (400 MHz, METHANOL-D4) δ 1.49-1.63 (m, 2 H), 1.65 (s, 9 H), 1.69-1.93 (m, 4 H), 1.98-2.19 (m, 4 H), 2.21-2.34 (m, 1 H), 3.73-3.82 (m, 4 H), 4.51 (d, J=7.42 Hz, 2 H), 7.84 (dd, J=8.59, 1.76 Hz, 1 H), 7.98 (d, J=8.59 Hz, 1 H), 8.13 (d, J=1.76 Hz, 1 H); MS (ESI) (M+H)+=426.2.

Provenance & Evidence