Electric Literature of 94838-59-2, A common heterocyclic compound, 94838-59-2, name is tert-Butyl 4-aminophenethylcarbamate, molecular formula is C13H20N2O2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
A mixture of l-methylpiperidine-4-carboxylic acid (500 mg, 3.49 mmol), HATU (1.59 g, 4T8mmol) and DIPEA (1.13 g, 8.73 mmol) in DCM (20 mL) was stirred at room temperature for 0.5 h. Then / -butyl 4-aminophenethylcarbamate (825 mg, 3.49 mmol) was added and the reaction was stirred at room temperature overnight. TLC showed the reaction completed. The reaction mixture was concentrated and purified by column chromatography to afford the title compound as white solid (170 mg, 13.5 % yield). ‘H NMR (500 MHz, DMSO-r/6) S: 9.75 (s, 1H), 7.49 (d, J= 8.4 Hz, 2H), 7.08 (d, J= 8.4 Hz, 2H), 6.82 (t, J= 5.3 Hz, 1H), 3.14 – 3.04 (m, 2H), 2.80 (d, J= 11.4 Hz, 2H), 2.62 (t, J= 7.5 Hz, 2H), 2.23 (ddd, J= 15.5, 7.8, 4.1 Hz, 1H), 2.15 (s, 3H), 1.91 – 1.79 (m, 2H), 1.66 (ddd, J= 17.6, 15.5, 6.7 Hz, 4H), 1.36 (s, 9H).
The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.
Reference:
Patent; ZHEJIANG VIMGREEN PHARMACEUTICALS, LTD; SUN, Sanxing; ZHAO, Long; HU, Chongbo; CHEN, Zhengshu; YE, Jinqi; (0 pag.)WO2020/2969; (2020); A1;,
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