With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.
Compound (e) (222.11 mg, 511.45 muiotaetaomicronIota, 1.5 eq.) was taken in a flask along with DMF as a solvent (approx. 1.5 mL per 1 mmol). (4-((4-methylpiperazin-l- yl)methyl)phenyl)methanamine (70 mg, 340.97 muiotaetaomicronIota, 1 eq.), HOBT (92.14 mg, 681.93 muiotatauiotaomicronIota, 2 eq.), and DIC (93.43 muIota_, 596.69 muiotaetaomicronIota, 1.75 eq.) were added respectively at room temperature and under N2. After 18 hours, the reaction was finished. The solution was quenched with water and then extracted with ethyl acetate. The organic layer was combined and dried with anhydrous MgS04 and concentrated in vacuo. The crude solid was purified through column chromatography using silica gel and eluent ethyl acetate and methanol (up to 2%). The product, 32, was obtained as a brown solid with 51% yield. (0153) FT-IR (Neat) : v (cm”1) = 2941, 2797, 1720, 1634, 1548, 1514, 1451, 1435, 1290, 1275, 1174, 1142, 1112; 1H-NMR (400 MHz, CDCI3) : delta ppm 7.98 (d, J = 9.1 Hz, 2H), 7.33 (s, 1H), 7.25 – 7.30 (m, 2H), 7.21 (d, J = 8.6 Hz, 2H), 6.89 (d, J = 8.6 Hz, 2H), 6.40 (t, J = 4.78 Hz, NH), 4.46 (d, J = 5.54 Hz, 2H), 3.91 (s, 3H), 3.33 (s, 3H), 3.18 – 3.24 (m, 4H), 2.55 – 2.62 (m, 4H), 2.36 (s, 3H) ; 13C-NMR (100 MHz, CDCI3) : delta 166.20, 159.32, 151.02, 144.67, 140.53, 136.40, 130.56, 129.23, 129.05, 127.84, 127.52, 127.33, 126.03 (2C), 116.11 (2C), 115.83 (2C), 55.01 (2C), 52.35 (2C), 48.87, 46.12, 43.76, 30.36; HRMS-ESI (m/z) : calcd. for C26H29BrN405S2 = 621.0763, found = 621.0828.
As the paragraph descriping shows that 216144-45-5 is playing an increasingly important role.
Reference£º
Patent; KING’S COLLEGE LONDON; THURSTON, David Edwin; KHONDAKER, Mirazur Rahman; JAMSHIDI, Shirin; NAHAR, Kazi Sharmin; (77 pag.)WO2019/30538; (2019); A1;,
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