With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.
630125-91-6, Example 69 Preparation of ethyl6-(3-(3-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1H-indazole-3-carboxylate To a stirred solution of 4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)benzeneamine (30.6 mg) in 1,4-dioxane (1 Ml), was added 4-nitrophenylchloroformate (21.6 mg) at room temperature. After 60 C. at 1 h, them mixture was cooled to rt and ethyl 6-(3-aminophenyl)-1H-indazole-3-carboxylate (30 mg) was added. The mixture was stirred at 90 C. for 12 h. Ethyl acetate and water were added and the aqueous layer was extracted with ethyl acetate three times. The combined organic layer was dried over magnesium sulfate and concentrated under reduced pressure. The residue was triturated in ethyl acetate/hexane to give 6-(3-(3-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)ureido)phenyl)-1H-indazole-3-carboxylate (16.2 mg). 1H NMR (400 MHz, DMSO-d6) delta13.98 (s, 1H), 9.09 (s, 1H), 8.93 (s, 1H), 8.15 (8.4 Hz, 1H), 7.99 (s, 1H), 7.93 (s, 1H), 7.81 (s, 1H), 7.62 (m, 3H), 7.43 (br d, J=4.4 Hz, 2H), 7.28 (m, 1H), 4.41 (q, J=7.2 Hz, 2H), 3.54 (s, 2H), 2.49 (m, 10H), 1.39 (t, J=7.2 Hz, 3H).
The synthetic route of 630125-91-6 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Sim, Tae Bo; Son, Jung Beom; Kim, Hwan; Park, Dong Sik; Choi, Hwan Geun; Ham, Young Jin; Hah, Jung Mi; Yoo, Kyung Ho; Oh, Chang Hyun; Lee, So Ha; Ha, Jae Du; Cho, Sung Yun; Kwon, Byoung Mog; Han, Dong Cho; US2012/130069; (2012); A1;,
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