(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-methoxyethyl)-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 (97 mg, 39% yield) as a brown solid was prepared according to the procedure described for Example 448, using 2-(tert-butylamino)-8-iodo-3-(2-methoxyethyl)quinazolin-4(3H)-one (715) (245 mg, 0.61 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) (208 mg, 0.79 mmol) as the starting materials. 1H NMR (400 MHz, DMSO-d6) δ ppm 11.95 (1H, br.), 7.90 (2H, m), 7.66 (1H, s), 7.20 (1H, t, J=7.7 Hz), 6.74 (1H, s), 6.51 (1H, s), 4.55 (1H, q, J=6.7 Hz), 4.28 (2H, m), 3.71 (2H, t, J=4.5 Hz), 3.36 (3H, s), 1.49 (9H, s), 1.38 (3H, d, J=6.7 Hz). m/z (ESI, +ve) 410.0 (M+H)+.

Provenance & Evidence