Some tips on (R)-1-Boc-3-Methylpiperazine

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

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 (500 mg, 2.50 mmol) , propionic acid (0.22 mL, 3.00 mmol) , EDCI (718 mg, 3.74 mmol) and HOAT (850 mg, 6.24 mmol) in DCM (15 mL) was stirred at 0 , and DIPEA (1.7 mL, 9.99 mmol) was added dropwise. After the addition, the mixture was stirred at rt for 16 h and washed with water (10 mL × 2) . 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 3-methyl-4-propionylpiperazine-1-carboxylate as colorless oil (630 mg, 95) .1H NMR (400 MHz, CDCl3) : delta ppm 4.76, 4.36 (m, m, 0.5H, 0.5H) , 4.00-3.94 (m, 1H) , 3.85-3.76 (m, 1H) , 3.53, 3.29 (m, m, 0.5H, 0.5H) , 2.98-2.96 (m, 1H) , 2.83-2.74 (m, 2H) , 2.34-2.26 (m, 2H) , 1.45 (s, 9H) , 1.13 (t, J 7.0 Hz, 6H) .

163765-44-4, 163765-44-4 (R)-1-Boc-3-Methylpiperazine 2756811, apiperazines compound, is more and more widely used in various fields.

Reference:
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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics