2-Bromo-1,3-thiazole-4-carboxamide → 2-[3-(6-tert-Butyl-1-oxo-1H-phthalazin-2-yl)-2-hydroxymethyl-phenyl]-thiazole-4-carboxylic acid amide

Participants

Reaction Steps

This compound was prepared with the same method as described in Example 1 by using 2-bromothiazole-4-carboxylic acid amide (intermediate-2) 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 (25% yield). 1H NMR (300 MHz, DMSO-d6): δ 8.56 (s, 1H), 8.41 (s, 1H), 8.24 (d, J=8.4 Hz, 1H), 8.05-8.00 (m, 2H), 7.82 (dd, J=1.8, 7.2 Hz, 1H), 7.61-7.58 (m, 2H), 4.54-4.45 (m, 2H), 1.41 (s, 9H). LC-MS calcd for C23H22N4O3S (m/e) 434.14, obsd 435 [M+1]+.

Provenance & Evidence