With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.132710-90-8,1-Boc-4-(3-hydroxypropyl)piperazine,as a common compound, the synthetic route is as follows.
[0974] A second intermediate compound, 4-[3-(7-Benzyloxy-[1,8]naphthyridin-2-yloxy)-propyl]-piperazine-1-carboxylic acid tert-butyl ester, was produced as follows: A 5 L 4-necked flask, equipped with a mechanical stirrer, thermometer, nitrogen inlet and an addition funnel is charged with a solution of 4-(3-hydroxy-propyl)-piperazine-1-carboxylic acid tert-butyl ester, (129 g, 0.528 mol) in anhydrous THF (1.6 L) and cooled to -40 C. To this potassium tert-butoxide solution (580 mL, 1M in THF, 0.58 mol) is added drop-wise during 1 h, and stirred further for 30 min. 2-Benzyloxy-7-chloro-[1,8]naphthyridine (130 g, 0.48 mol) is added to the reaction mixture in portions at -40 C. during 1 h. The reaction is stirred for 4 h to bring to 0 C., then quenched with saturated ammonium chloride solution (1.5 L) and extracted with ethyl acetate (2 L and 1 L). The combined organic extracts are washed with brine (1 L), dried over anhydrous sodium sulfate and concentrated to afford the crude as a dark brown thick paste. The crude is purified by silica gel chromatography using 20-25% ethyl acetate in hexanes for elution to give the second intermediate compound as a thick almost colorless thick paste (126 g, 49.8%).
132710-90-8, 132710-90-8 1-Boc-4-(3-hydroxypropyl)piperazine 16217800, apiperazines compound, is more and more widely used in various.
Reference£º
Patent; Clark, Jerry D.; Davis, Jamie M.; Favor, David; Fay, Lorraine K.; Franklin, Lloyd; Henegar, Kevin E.; Johnson, Douglas S.; Nichelson, Brian J.; Ou, Ligong; Repine, Joseph Thomas; Walters, Michael A.; White, Andrew David; Zhu, Zhijian; US2005/43309; (2005); A1;,
Piperazine – Wikipedia
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