Analyzing the synthesis route of tert-Butyl 2-methylpiperazine-1-carboxylate

120737-78-2, The synthetic route of 120737-78-2 has been constantly updated, and we look forward to future research findings.

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;,
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