With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.120737-78-2,tert-Butyl 2-methylpiperazine-1-carboxylate,as a common compound, the synthetic route is as follows.
A suspension of 7-bromo-2-(5-chloro-2,4-dimethoxyphenyl) imidazo[ l,2-a] pyridine 22 (200 nig, 0.544 rnmol), tert-butyl 2-methylpiperazine-1-carboxylate 202 (218 mg, 1.09 mmol), Xanthphos (34 mg, 0.059 mmol) and t-BuOK ( 181 n g, 1.62 mmol) in toluene (10 mL) was degassed with argon for 5 min. Subsequently the mixture was charged with Pd 2(dba)3 (24 mg, 0.026 mmol) and again degassed with argon for another 5 min. The resulting reaction mixture was heated at 100-1 10 C for 16 h. The reaction mixture was cooled, filtered through a pad of celite and evaporated to dryness. The residue obtained was purified by combi-flash companion (silica gel, CH3OH/CH2CI2) to provide tert-butyl 4-(2-(5-chloro-2,4-dimethoxyphenyl)-imidazo[1,2-a]pyridin-7-yl)-2-methylpiperazine-1-carboxylate 203 (90 mg, 34%) as an off-white solid. 1HNMR (400MHz, DMSO-d6): delta 8.32 (d, J=7.6Hz, III).8.16 (s. III).8.02 (s, 1H), 6.86 (s, 1H), 6.78 (dd, J= 2.4, 7.6 Hz, ii).6.66 (d, J= 1.6 Hz, 1H), 4.22-4.20 (m, IH), 4.00 (s, 3H), 3.93 (s, 3H), 3.83-3.79 (m, IH), 3.70 -3.60 (m, 2H), 3.22-3.16 (m, ill). 2.97-2.91 (m, IH), 2,76-2,70 (m, III).1.42 (s, 9H), 1.18 (d, ./ 6.4 Hz, 3H); HPLC (Method 6) 97.0% (AUC), = 14.23 min.; ESI-APCl MS m/z 487 [M + HI .
120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ONCOTHERAPY SCIENCE, INC.; MATSUO, Yo; HISADA, Shoji; NAKAMURA, Yusuke; CHAKRABARTI, Anjan; RAWAT, Manish; RAI, Sanjay; SATYANARAYANA, Arvapalli, Venkata; DUAN, Zhiyong; TALUKDAR, Arindam; RAVULA, Srinivas; DECORNEZ, Helene; (491 pag.)WO2017/58503; (2017); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics