With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1019351-46-2,Methyl 4-aminopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.
200 g of tetrahydrofuran was placed in a 500 ml four-necked flask equipped with a stirring and a thermometer.12.5 g (0.05 mol) of (2S,5R)-5-benzyloxyaminopiperidine-2-carboxylic acid, 50 g of tri-n-butylamine,0.1 g of N,N-dimethylformamide, cooled at -10 C,A mixed solution of 23.8 g (0.08 mol) of solid phosgene and 80 g of tetrahydrofuran was added dropwise.The reaction was stirred at 10-20 C for 4 hours.Between 10 and 20 C, a mixed solution of 11.0 g (0.07 mol) of 1-methoxycarbonyl-4-aminopiperidine and 30 g of tetrahydrofuran was added.Stir the reaction between 15-20 C for 3 hours.The reaction liquid was poured into 300 g of ice water mixture and layered.The aqueous layer was extracted twice with dichloromethane, 50 g each time.The organic phases were combined and washed twice with saturated sodium chloride solution, 20 g each time.After the obtained organic phase recovers the solvent,18.2 g of (2S,5R)-N-(1-(methoxycarbonyl)piperidin-4-yl)-6-benzyloxy-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamide ,The liquid phase purity was 99.8%, and the yield was 93.3%., 1019351-46-2
The synthetic route of 1019351-46-2 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; Xin Fa Pharmaceutical Co., Ltd.; Qi Yuxin; Li Xinfa; Wang Baolin; Xu Xin; Zhao Yinlong; Teng Yuqi; (9 pag.)CN109928970; (2019); A;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem