With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.414910-15-9,tert-Butyl 4-(cyclopropanecarbonyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,414910-15-9
Preparation of N-cyclopropanoyl piperazinium p-toluenesulfonate (compound A) N-Boc-4-cyclopropanoyl piperazine (20.00 g, 78.64 mmol, 1.0 equiv.) and p-toluenesulfonic acid (p-TSA) monohydrate (15.71 g, 82.60 mmol, 1.05 equiv.) and ethyl acetate (EtOAc) (160 mL, 8 vol.) were added to a 3-necked 250 mL flask equipped with 5 cm stir bar, condenser, thermal couple and N2 inlet. The resulting mixture was heated to 50 C. overnight. The reaction was monitored by TLC. Upon completion, the suspension was cooled to 0 C. in ice bath and stirred for 1 hour. After stirring, the resulting slurry was filtered through Buchner funnel. The obtained wet cake was washed with EtOAc (20.0 mL, 1 vol.) twice (and dried at not more than 60 C. under vacuum overnight to afford compound A as white solid (23.12 g, 70.83 mmol, 90.08% Yield). 1H NMR (400 MHz, CDCl3) ?: 0.75 (m, 2H), 0.94 (m, 2H), 1.61 (m, 1H), 2.35 (s, 3H), 3.23 (br, 4H), 3.86 (br, 4H), 7.19 (d, J=8.2 Hz, 2H), 7.69 (d, J=8.2 Hz, 2H), 9.20 (br, 1H).
The synthetic route of 414910-15-9 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; SCINOPHARM TAIWAN, LTD.; HSIAO, Tsung-Yu; CHANG, Yung-Hung; (16 pag.)US2018/57464; (2018); A1;,
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