Downstream synthetic route of (4-Aminophenyl)(4-methylpiperazin-1-yl)methanone

As the paragraph descriping shows that 55121-99-8 is playing an increasingly important role.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.55121-99-8,(4-Aminophenyl)(4-methylpiperazin-1-yl)methanone,as a common compound, the synthetic route is as follows.

55121-99-8, A mixture of tert-butyl tert-butyl N-[(1r,4r)-4-[(6-chloro-5-cyanopyrazin-2- yl)amino]cyclohexyl]carbamate (0.3 g, 0.89 mmol), methylpiperazine-1-carbonyl)aniline (0.39 g, 1.77 mmol), Pd(OAc)2 (40 mg, 0.177 mmol), (+/-) BINAP (110 mg, 0.177 mmol), fine powder Cs2CO3 (0.87 g, 2.67 mmol) in dioxane (50 mL) was degassed with a nitrogen stream for 10 min. The mixture was stirred in a nitrogen atmosphere at 110C overnight, then cooled to room temperature and concentrated in vacuo. The residue was purified by flash chromatography with 20 to 100% ethyl acetate in cyclohexane to give tert-butyl tert-butyl N-[(1r,4r)-4-[(5-cyano- 6-{[4-(4-methylpiperazine-1-carbonyl)phenyl]amino}pyrazin-2-yl)amino]cyclohexyl]carbamate (0.289 g, 61% yield). MS found for C28H38N8O3 as (M+H)+ 535.18.

As the paragraph descriping shows that 55121-99-8 is playing an increasingly important role.

Reference:
Patent; PHARMACYCLICS LLC.; ATALLAH, Gordana, Babic; CHEN, Wei; JIA, Zhaozhong, J.; POZZAN, Alfonso; RAVEGLIA, Lucal, Francesco; ZANALETTI, Riccardo; (815 pag.)WO2016/196776; (2016); A2;,
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