With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59878-57-8,1-(Cyclopropylcarbonyl)piperazine,as a common compound, the synthetic route is as follows.
To the solution of 124 mg (0.357 mmol) of Intermediate II-1 in 4.0 ml of dry DCM, 69.5 mg (0.428 mmol) 1-(cyclopropylcarbonyl)piperazine were added and then stirred at room temperature. After 1 h, 151 mg (0.714 mmol) of sodium triacetoxyborohydride were added and stirring was continued at room temperature for further 1 h. Water was added to the reaction mixture and phases were separated. Aqueous phase was extracted 3x with chloroform. Combined organic phases were dried over anhydrous sodium sulphate. After filtration of the drying agent and evaporation of the solvent under reduced pressure, the residue was purified on a chromatographic plate. CHCl3/MeOH 90/10 system was used for separation. After separation, 170 mg (98%) of the compound 1 were obtained. 1H NMR (300 MHz, CDCl3) delta 8.55 (bs; 1H); 7.61 (dd; J = 7.4; 0.8 Hz; 1H); 7.52 – 7.47 (m; 1H); 7.36 – 7.27 (m; 2H); 7.13 – 7.08 (m; 1H); 6.66 (s; 1H); 6.64 (s; 1H); 4.03 – 3.95 (m; 4H); 3.84 (s; 2H); 3.81 – 3.65 (m; 8H); 2.71 – 2.53 (m; 4H); 1.81 – 1.70 (m; 1H); 1.02 – 0.95 (m; 2H); 0.79 – 0.71 (m; 2H). MS-ESI: (m/z) calculated for C27H31N7O2 [M+H]+: 486.59; determined 486.2.
59878-57-8, The synthetic route of 59878-57-8 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; CELON PHARMA S.A.; DYMEK, Barbara; ZAGOZDA, Marcin; WIECZOREK, Maciej; DUBIEL, Krzysztof; STANCZAK, Aleksandra; ZDZALIK, Daria; GUNERKA, Pawel; SEKULAR, Mariola; DZIACHAN, Maciej; (70 pag.)WO2016/157091; (2016); A1;,
Piperazine – Wikipedia
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