Azetidine → HCID 178508625, compound

Participants

Reaction Steps

The DMF (3 mL) solution of cis-toluene-4-sulfonic acid 3-(4-amino-5-iodopyrrolo[2,3-d]pyrimidin-7-yl)-cyclobutylmethyl ester (see above for its preparation) (63 mg, 80% purity, 0.10 mmol) and azetidine (12 mg, 2 eq.) was stirred at 50° C. overnight in a sealed tube. The reaction mixture was used directly for further reaction. MS (ES+): 384.1 [MH+]. HPLC: tR=1.4 min (polar—5 min). For 1H NMR analysis, a small sample was taken out for HPLC purification. 1H NMR (DMSO-d6, 400 MHz): δ=1.99-2.06 (quintet, 2 H, J=6.9 Hz), 2.08-2.22 (m, 3 H), 2.49-2.53 (m, 2 H), 2.54-2.56 (d, 2 H, J=6.4 Hz), 3.15-3.19 (d, 4 H, J=7.2 Hz), 5.01-5.10 (quintet, 2 H, J=8.7 Hz), 6.69 (brs, 2 H), 7.80 (s, 1 H), 8.16 (s, 1 H).

Provenance & Evidence