Reference of 1062368-71-1 ,Some common heterocyclic compound, 1062368-71-1, molecular formula is C9H7BrN2O2, 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.
Methyl 4-bromopyrazolo [1,5 -a]pyridine-3 -carboxylate (100 mg, 0.39 mmol), Pd(OAc)2 (5.3 mg, 0.024 mmol), BNAP (22 mg, 0.035 mmol) and Cs2CO3 (192 mg, 0.59 mmol) were placed in a pressure vial. The reaction mixture was degassed (3x vacuum and argon), then toluene (2 mL) and morpholine (0.044 mL, 0.51 mmol) were added. Thereaction mixture was degassed again, and then was stirred at 120 C for 3 h. After cooled to rt, the reaction was filtered through a pad of CELITE, and the solvent was removed. The crude product was purified by reverse phase chromatography to provide Intermediate 109 (74 mg, 72%) as a light tan solid. ?H NMR (400MHz, CDC13) oe 8.46 (s, 1H), 8.43 (d, J=6.6 Hz, 1H), 7.31 (d, J=7.7 Hz, 1H), 7.05 (t, J7.2 Hz, 1H), 4.11 – 4.04(m, 4H), 3.94 (s, 3H), 3.40 – 3.27 (m, 4H). LC-MS(ESI) m/z: 262.0 [M+H].
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,1062368-71-1, its application will become more common.
Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; LADZIATA, Vladimir; GLUNZ, Peter W.; HU, Zilun; WANG, Yufeng; (0 pag.)WO2016/10950; (2016); A1;,
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