With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.189333-49-1,3-Benzyl-3,9-diazaspiro[5.5]undecane,as a common compound, the synthetic route is as follows.
Example 8D (500 mg, 2.05 mmol) and Boc2O (450 mg, 2.06 mmol) in methanol mixture was added triethylamine (311 mg, 3.08 mmol) and the mixture was stirred at 20-30 deg.C for 16 hours. The reaction mixture was concentrated, and the residue was diluted with ethyl acetate (20 mL), and washed with water (15mL × 2) and brine (20 mL) was washed, and the organic layer was dried over anhydrous sodium sulfate, and concentrated. The crude intermediate was dissolved in ethanol (15mL) and acetic acid (2mL), followed by addition of palladium hydroxide / carbon (0.1 g). The mixture was reacted under hydrogen (50Psi) for 20 hours. The mixture was filtered, the filtrate was concentrated to give the acetate salt (320 mg, 1.26 mmol, 61.37% yield) of the title compound., 189333-49-1
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Reference：
Patent; Nanjing Mingde New Drug Research and Development Co. Ltd.; Qilu Pharmaceutical Co., Ltd.; Ding, Zhaozhong; Zhang, Minghui; Chen, Shuhui; Liu, Xile; Zhu, Yidong; Fan, Chuanwen; Zhao, Baoping; Zhang, Long; Chen, Dong; Yang, Yingying; Zheng, Qingmei; Zheng, Shansong; Wan, Haiwen; Hu, Jinqing; (93 pag.)CN105330698; (2016); A;,
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