Analyzing the synthesis route of 163765-44-4

The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.163765-44-4,(R)-1-Boc-3-Methylpiperazine,as a common compound, the synthetic route is as follows.

A mixture of (R) -tert-butyl 3-methylpiperazine-1-carboxylate (300 mg, 1.5 mmol) , butyric acid (200 mg, 2.3 mmol) , EDCI (595 mg, 3.0 mmol) and HOAT (306 mg, 2.3 mmol) in DCM (10 mL) was stirred at 0 , and DIPEA (0.76 mL, 4.5 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 10 h and washed with water (10 mL ¡Á 3) . The organic layer was dried over anhydrous Na2SO4 and concentrated. The residue was purified by silica gel chromatography eluted with Petroleum ether/EtOAc (v/v) 2/1 to give (R) -tert-butyl 4-butyryl-3-methylpiperazine-1-carboxylate as colorless liquid (370 mg, 91) .1H NMR (600 MHz, CDCl3) : delta ppm 4.74-4.81, 4.34-4.41 (m, 0.5H, 0.5H) , 3.80-4.12, 3.53-3.60 (m, 2.5H, 0.5H) , 3.26-3.35, 2.75-2.98 (m, 0.5H, 2.5H) , 2.26-2.35 (m, 2H) , 1.61-1.69 (m, 2H) , 1.47 (s, 9H) , 1.13-1.24 (m, 3H) , 1.12 (t, J 7.3 Hz, 3H) and MS-ESI: m/z 215.10 [M-55] +., 163765-44-4

The synthetic route of 163765-44-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Yingjun; LIU, Bing; YU, Tianzhu; ZHANG, Xiangyu; ZHANG, Shiguo; ZHANG, Jiancun; CHENG, Changchung; (426 pag.)WO2016/34134; (2016); A1;,
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