342417-01-0

Hazard Information

Synthesis

109-01-3

342417-00-9

342417-01-0

Step 3: 1.0 g (4.05 mmol) of 6-chloro-4-o-tolylnicotinamide was dissolved in 9.0 mL of N-methylpiperazine, heated to 100 °C and the reaction was maintained for 2 hours. Upon completion of the reaction, the excess N-methylpiperazine was removed by high vacuum distillation. The residue was purified by silica gel column chromatography using dichloromethane as eluent to give 1.2 g (95% yield) of the target compound, 6-(4-methylpiperazin-1-yl)-4-(o-tolyl)nicotinamide, the product was a pale yellow crystalline foam. Mass spectrometry (ISP): m/z 311 ([M+H]+, 100%), 254 (62%).

References

[1] Patent: US8426450, 2013, B1. Location in patent: Page/Page column 25
[2] Patent: US9403772, 2016, B2. Location in patent: Page/Page column 30
[3] Journal of Organic Chemistry, 2006, vol. 71, # 5, p. 2000 - 2008
[4] Patent: JP2015/17121, 2015, A. Location in patent: Paragraph 0153

Questions And Answer

• Application

  Netupitant is a selective antagonist of the human substance P/neurokine 1 (NK1) receptor. Panostron is a 5-HT3 receptor antagonist with a strong binding affinity for this receptor and low or no affinity for other receptors. 6-(4-methylpiperazin-1-yl)-4-(2-methylphenyl)nicotinamide is an organic synthesis intermediate and pharmaceutical intermediate used in laboratory research and development processes and chemical and pharmaceutical synthesis, primarily as an intermediate for netupitant.;

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