(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-(4-oxo-1,4,5,6-tetrahydropyrrolo[3,4-b]pyrrol-2-yl)-4(3H)-quinazolinone

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Reaction Steps

This compound (138 mg, 51% 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) (273 mg, 0.68 mmol) and 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyrrolo[3,4-b]pyrrol-4(1H)-one (706) (219 mg, 0.88 mmol) as the starting materials. 1H NMR (400 MHz, DMSO-d6) δ ppm 12.09 (1H, br.), 7.90 (2H, m), 7.56 (1H, br.), 7.20 (1H, t, J=7.4 Hz), 6.83 (1H, s), 6.50 (1H, s), 4.27 (4H, m), 3.70 (2H, m), 3.35 (3H, s), 1.49 (9H, s). m/z (ESI, +ve) 395.9 (M+H)+.

Provenance & Evidence