Synthetic Route of 327-51-5, A common heterocyclic compound, 327-51-5, name is 1,4-Dibromo-2,5-difluorobenzene, molecular formula is C6H2Br2F2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
(1380) [00444] Into a 50-mL round-bottom flask that was purged and maintained under an inert atmosphere of nitrogen was added 1 ,4-dibromo-2,5-difiuorobenzene (1.50 g, 5.52 mmol), tert- butyl 4-(tetramethyl-l,3,2-dioxaborolan-2-yl)-l,2,3,6-tetrahydropyridine-l-carboxylate (1.88 g, 6.06 mmol), potassium carbonate (2.28 g, 16.5 mmol), Pd(dppf)Cb’CH2Cl2 (400 mg, 0.49 mmol), DMF (20 mL) and H2O (2 mL). The reaction mixture was stirred for 2 h at 50 C and then cooled and quenched with water (20 mL). The resulting solution was extracted with ethyl acetate (3 x 50 mL). The combined organic layers were washed with water (50 mL) and brine (50 mL). The organic layer was then concentrated in vacuo. The resulting crude product was purified by FCC eiuting with petroleum ether/ethyl acetate (5: 1) to afford fer/-butyl 4-(4-bromo- 2,5-difluorophenyl)-3,6-dihydropyridine-l(2 )-carboxylate (1.5 g, 73%). H-NMR (300 M ( DO delta ppm 7.21-7.29 (m, 1H), 6.93-7.08 (m, 1H), 5.81-5.61 (m, 1H), 4.01-4.14 (m, 2H), 3.62 (t, J – 5,7 Hz, 2H), 2.48-2.51 (m, 2H), 1 ,50 (s, 9H).
The synthetic route of 327-51-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; FORMA THERAPEUTICS, INC.; GUERIN, David Joseph; BAIR, Kenneth W.; CARAVELLA, Justin A.; IOANNIDIS, Stephanos; LANCIA JR., David R.; LI, Hongbin; MISCHKE, Steven; NG, Pui Yee; RICHARD, David; SCHILLER, Shawn E. R.; SHELEKHIN, Tatiana; WANG, Zhongguo; (365 pag.)WO2017/139778; (2017); A1;,
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