4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-2-fluoro-5-methoxybenzoic acid → 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[5,4-b][1,4]diazepin-2-ylamino)-2-fluoro-5-methoxy-N-(3-((4-methylpiperazin-1-yl)methyl)phenyl)benzamide

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Reaction Steps

The title compound was prepared in a manner analogous to compound 149 from 4-(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[5,4-b][1,4]diazepin-2-ylamino)-2-fluoro-5-methoxybenzoic acid and 3-((4-methylpiperazin-1-yl)methyl)aniline hydrochloride with yield 43 mg (33%). 1H NMR (400 MHz, DMSO-d6) δ ppm 1.62 (br. s., 6 H) 1.99 (br. s., 2 H) 2.14 (s, 3 H) 2.33 (br. s., 8 H) 3.43 (s, 2 H) 3.94 (s, 3 H) 4.09 (t, J=13.89 Hz, 2 H) 4.84 (br. s., 1 H) 7.01 (d, J=7.58 Hz, 1 H) 7.20-7.35 (m, 2 H) 7.61 (br. s., 1 H) 7.67 (br. s., 1 H) 8.10 (s, 1 H) 8.23-8.40 (m, 2 H) 10.14 (s, 1 H). [M+H] calc'd for C33H39F3N8O3, 653; found 653.

Provenance & Evidence