Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 1436686-17-7, name is Ethyl 5-bromopyrazolo[1,5-a]pyrimidine-3-carboxylate. A new synthetic method of this compound is introduced below., HPLC of Formula: C9H8BrN3O2
To a solution of cyclopropylboronic acid (174mg, 2.1mmol), KOAc (330mg, 3.4mmol), ethyl 5-bromopyrazolo[l,5-a]pyrimidine-3-carboxylate (500mg, 1.7mmol) in dioxane (15ml) was added PdCl2(dppf).DCM (138mg, 0.17mmol). The reaction mixture was stirred at 90 C for 2.5 h under a nitrogen atmosphere and then concentrated in vacuo. The residue was diluted with water and then extracted with DCM (20 x 3). The combined organic layers were washed with brine and dried over anhydrous Na2S04, filtered and concentrated in vacuo. The residue was purified by a silica gel column chromatography (DCM/EA (v/v) = 6/1) to give the title compound as a brown solid (220 mg, 57%). H NMR (300 MHz, CDC1 ): delta (ppm) 8.51 (d, J = 7.2 Hz, 1H), 8.47 (s, 1H), 6.78 (d, J = 7.2 Hz, 1H), 4.39 (q, J= 7.1 Hz, 2H), 2.25-2.16 (m, 1H), 1.41 (t, J= 7.1 Hz, 3H), 1.33-1.25 (m, 2H), 1.25- 1.14 (m, 2H).
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Reference:
Patent; CALITOR SCIENCES, LLC; SUNSHINE LAKE PHARMA CO., LTD.; XI, Ning; LI, Minxiong; LI, Xiaobo; WO2015/73267; (2015); A1;,
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