Ammonia → HCID 86678984, compound

Participants

Reaction Conditions

Reaction Steps

Ammonia (2.0M in MeOH, 11 mL, 22 mmol) was added to ethyl 4-amino-2-[6-chloro-1-(3,3,4,4,4-pentafluorobutyl)-1H-indazol-3-yl]-5-methyl-6-oxo-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine-5-carboxylate, as prepared by the procedure described in Example 157, (150 mg, 0.289 mmol, single enantiomer from SFC separation on Chiralpak AD column). The resultant mixture was heated at 50° C. for 16 hours. The reaction solution was then concentrated in vacuo, and the residue purified by preparative TLC using 5% MeOH in DCM (with 0.5% NH4OH) as the eluent to give the indicated compound. 1H NMR (500 MHz, DMSO-d6): δ 8.66 (d, J=8.7 Hz, 1H); 8.02 (d, J=1.4 Hz, 1H); 7.45 (br s, 1H); 7.27 (dd, J=8.7, 1.7 Hz, 1H); 7.19 (br s, 1H); 6.79 (br s, 2H); 4.82 (t, J=6.8 Hz, 2H); 2.95-2.85 (m, 2H); 1.56 (s, 3H). m/z=504.1 (M+H).

Provenance & Evidence