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. 1224944-77-7, name is Ethyl 5-chloropyrazolo[1,5-a]pyrimidine-3-carboxylate. A new synthetic method of this compound is introduced below., Recommanded Product: 1224944-77-7
To a solution of (tf)-2-(l-aminoethyl)-4-fluorophenol (2) (85 g, 443.56 mmol, 1.00 eq.) and ethyl 5-chloropyrazolo[l,5-a]pyrimidine-3-carboxylate (la) (100.08 g, 443.56 mmol, 1.00 eq.) in n-BuOH (2 L) was added DIEA (343.96 g, 2.66 mol, 6.00 eq.). The mixture was stirred at 120 C for 2 hrs. TLC (PE:EtOAc=l : l) showed the reaction was completed. The reaction mixture was diluted with H20 (500 mL) at 16 C, and extracted with EtOAc (500 mLx3). The combined organic layers were washed with brine (500 mL), dried over Na2S04, filtered and concentrated under reduced pressure to give a residue. The residue was purified by column chromatography (Si02, Petroleum ether/Ethyl acetate=10/l to 1 :3) to give ethyl (K)-5-((l-(5- fluoro-2-hydroxyphenyl)ethyl)amino)pyrazolo[l,5-a]pyrimidine-3-carboxylate (3) (122 g, 349.34 mmol, 78.76% yield, ee>99% purity) as a white solid. 1HNMR (CDC13 , 400MHz) delta 9.28 (br. s., IH), 8.26 (s, IH), 8.14 (d, 7=7.5 Hz, IH), 6.95 – 6.89 (m, 2H), 6.87 – 6.80 (m, IH), 6.18 (d, 7=7.5 Hz, IH), 5.98 (d, 7=8.3 Hz, IH), 5.71 – 5.54 (m, IH), 4.50 – 4.35 (m, 2H), 1.60 (d, 7=6.8 Hz, 3H), 1.42 (t, J=7.2 Hz, 3H).
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Reference:
Patent; TP THERAPEUTICS, INC.; CUI, Jingrong Jean; LI, Yishan; ROGERS, Evan W.; ZHAI, Dayong; DENG, Wei; HUANG, Zhongdong; (120 pag.)WO2017/15367; (2017); A1;,
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