(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 → 2-(tert-butylamino)-3-(2-(2-methoxyethoxyl)ethyl)-8-((6R)-6-methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4-b]pyrrol-2-yl)-4(3H)-quinazolinone

Participants

Reaction Steps

This compound (102 mg, 40% yield) as a tan amorphous solid was prepared according to the procedure described for Example 448, using 2-(tert-butylamino)-8-iodo-3-(2-(2-methoxyethoxyl)ethyl)quinazolin-4(3H)-one (716) (250 mg, 0.56 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) (178 mg, 0.68 mmol) as the starting materials. 1H NMR (400 MHz, MeOH-d4) δ ppm 7.99 (2H, dd, J=7.6, 1.8 Hz), 7.23 (1H, t, J=7.7 Hz), 6.75 (1H, s), 4.69 (1H, q, J=6.8 Hz), 4.27-4.38 (2H, m), 3.90 (2H, t, J=4.3 Hz), 3.67-3.74 (2H, m), 3.55-3.63 (2H, m), 1.60 (9H, s), 1.52 (3H, d, J=6.8 Hz), 1.22 (6H, s). m/z (ESI, +ve) 454.0 (M+H)+.

Provenance & Evidence