1030377-21-9

(S)-1-Boc-2-(Hydroxymethyl)piperazine reacts with 1,2-difluoro-4-nitrobenzene to synthesize tert-butyl (S)-4-(2-fluoro-4-nitrophenyl)-2-(hydroxymethyl)piperazine-1-carboxylate. This compound serves as a crucial intermediate in the preparation of the Wee-1 kinase activity inhibitor.

To a solution of (S)-4-benzyl 1-tert-butyl 2-(hydroxymethyl)piperazine-1,4-dicarboxylate (1.5 g, 4.28 mmol) in MeOH (20 mL), 10 % Pd/C (150 mg) was added. The mixture was stirred at room temperature for 3 hours under H2. Afterwards, the solid was removed by filtration and the filtrate was concentrated to yield (S)-1-Boc-2-(Hydroxymethyl)piperazine (850 mg, 3.93 mmol, 91.82 percent) as a white solid.

[1] Patent: US2018/127370, 2018, A1. Location in patent: Paragraph 1006; 1004