4-bromo-1-methyl-1H-pyrrole-2-carboxylic acid amide → 4-[3-(6-tert-Butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-2-hydroxymethyl-phenyl]-1-methyl-1H-pyrrole-2-carboxylic acid amide

Participants

Reaction Steps

This compound was prepared with the same method as described in Example 1 by using 4-bromo-1-methyl-1H-pyrrole-2-carboxylic acid amide (intermediate-3) and acetic acid 2-(6-tert-butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-6-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzyl ester (intermediate 5). The desired compound was prepared in two steps (60% yield). 1H NMR (300 MHz, d6-DMSO) δ 8.49-8.48 (m, 1H), 7.86 (s, 1H), 7.73 (d, J=13.2 Hz, 1H), 7.44-7.42 (m, 3H), 7.25-7.23 (m, 2H), 7.06 (br s, 2H), 4.56 (s, 1H), 4.36 (s, 2H), 3.88 (s, 3H), 1.37 (s, 9H). LC-MS calcd for C25H25FN4O3 (m/e) 448.19, obsd 449.1 [M+H]+.

Provenance & Evidence