(R)-6-methyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyrrolo[3,4-b]pyrrol-4(1H)-one → 3-methyl-2-((1-methylcyclopropyl)amino)-8-((6R)-6-methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4-b]pyrrol-2-yl)-4(3H)-quinazolinone

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Reaction Steps

This compound (85 mg, 52% yield) as a brown solid was prepared according to the procedure described for Example 448, using 8-iodo-3-methyl-2-((1-methylcyclopropyl)amino)quinazolin-4(3H)-one (713) (160 mg, 0.45 mmol) and (R)-6-methyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyrrolo[3,4-b]pyrrol-4(1H)-one (705) (130 mg, 0.50 mmol) as the starting materials. 1H NMR (400 MHz, DMSO-d6) δ ppm 13.02 (1H, br.), 8.13 (1H, dd, J=7.6, 1.4 Hz), 7.83 (1H, dd, J=7.8, 1.4 Hz), 7.69 (2H, d, J=3.1 Hz), 7.18 (1H, t, J=7.7 Hz), 6.96 (1H, s), 4.64 (1H, q, J=6.6 Hz), 3.40 (3H, s), 1.56 (3H, s), 1.37 (3H, d, J=6.7 Hz), 1.01 (2H, m), 0.86 (2H, m). MS (ESI, pos. ion) m/z: 364.0 (M+1).

Provenance & Evidence