4-bromo-1-methyl-1H-pyrrole-2-carboxylic acid amide → 4-[3-(6-tert-Butyl-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-1-oxo-1H-phthalazin-2-yl)-6-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzyl ester (intermediate 4). The desired compound was prepared in two steps (20% yield). 1H NMR (300 MHz, DMSO-d6) δ 8.54 (s, 1H), 8.25 (d, J=8.4 Hz, 1H), 8.04 (d, J=1.5 Hz, 1H), 8.01 (dd, J=1.8, 8.4 Hz, 1H), 7.48-7.45 (m, 2H), 7.28-7.23 (m, 2H), 7.08 (d, J=1.8 Hz, 1H), 4.35 (s, 2H), 3.89 (s, 3H), 1.41 (s, 9H). LC-MS calcd for C25H26N4O3 (m/e) 430.20, obsd 431 [M+1]+.

Provenance & Evidence