(2,4-Dimethoxypyrimidin-5-yl)boronic acid → HCID 86703224, compound

Participants

Reaction Steps

The title compound was prepared in analogy to the procedure described for Example 125 but in the step corresponding to Step 125.1, 4-{2-bromo-5-[5-chloro-1-(4-methoxy-benzyl)-2-oxo-1,2-dihydro-pyridin-3-yl]-1-isopropyl-4-oxo-1,4,5,6-tetrahydro-pyrrolo[3,4-b]pyrrol-6-yl}-2-fluoro-benzonitrile (Intermediate BE) and 2,4-dimethoxypyrimidine-5-boronic acid were used instead of 4-{2-bromo-5-[5-chloro-1-(4-methoxy-benzyl)-2-oxo-1,2-dihydro-pyridin-3-yl]-1-isopropyl-4-oxo-1,4,5,6-tetrahydro-pyrrolo[3,4-b]pyrrol-6-yl}-benzonitrile and 4-methoxy-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyrimidin-2-ylamine respectively. Moreover, in this step, Pd(PPh3)4 was used instead of PdCl2(dppf).CH2Cl2 adduct. The title compound was obtained as a white solid. tR: 5.84 min (H PLC 2); ESI-MS: tR=0.94 min, [M+H]+ 549/551 (LC-MS 1); TLC: Rf=0.19 (EtOAc).

Provenance & Evidence