With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.
Sodium hydride (0.86 g, 21 mmol) was added to fert-butyl (3S)-3-(hydroxymethyl)piperazine-l-carboxylate (1.244 g, 5.75 mmol) in THF (40 ml) at rt. The resulting mixture was stirred at rt for 10 min. 7-Bromo-8-chloro-5,6-difluoroquinazolin-4-ol (1.7 g, 5.75 mmol) was added slowly and the resulting solution was stirred at 40C for 1 h. The reaction mixture was quenched with water (2 ml). The reaction mixture was adjusted to pH = 7 with 2M HCI. The crude product was purified by C18-flash chromatography (0 to 65% MeOH in water (0.1% TFA)) to afford ferf-butyl (3S)-3-{[(7-bromo-8-chloro-6-fluoro-4-hydroxyquinazolin-5-yl)oxy]methyl}piperazine-l-carboxylate (1.65 g, 58%) as a brown solid. XH NMR (400 MHz, DMSO) 1.35 (9H, s), 2.62-3.07 (2H, m), 3.11-3.19 (2H, m), 3.20-3.76 (1H, m), 3.80-3.88 (1H, m), 3.98-4.29 (3H, m), 8.23 (1H, s). m/z: ES+ [M+H]+ = 491., 314741-40-7
The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; LAMONT, Scott, Gibson; KEMMITT, Paul, David; GOLDBERG, Frederick, Woolf; (158 pag.)WO2019/215203; (2019); A1;,
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