With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.129799-15-1,Methyl 1-Boc-piperazine-2-carboxylate,as a common compound, the synthetic route is as follows.
Step 1 : 1-tert-Butyl 2-methyl 4-(4-fluorophenyl)piperazine-l,2-dicarboxylate (1113) [00386] To a solution of A29-1 (200.00 mg, 0.819 mmol, 1.00 eq) in DCM (5 mL) were added A29-1A (229. 11 mg, 1.64 mmol, 2.00 eq), Cu(OAc)2 (148.70 mg, 0.819 mmol, 1.00 eq), 4A MS (50 mg) and pyridine (0. 13 mL, 1.64 mmol, 2.00 eq). The reaction mixture was stirred at 25 C for 16 hours under oxygen atmosphere. The reaction mixture was concentrated under reduced pressure. The residue was purified by column chromatography over silica gel (petroleum ether: ethyl acetate = 1 :0 to 10: 1) to afford the title compound (250 mg, 90% yield). LCMS (ESI): RT = 0.800 min, mass calcd. for C17H23FN2O4 338.16, m/z found 338.9 [M+H] , NMR (400MHz, COCh-d) delta 7.00 – 6.93 (m, 2H), 6.91 – 6.84 (m, 2H), 4.92 – 4.85 (m, 0.5H), 4.73 – 4.66 (m, 0.5H), 4.09 – 3.88 (m, 2H), 3.78 (s, 3H), 3.40 – 3.18 (m, 2H), 2.94 – 2.83 (m, 1H), 2.79 – 2.66 (m, 1H), 1.49 (d, J=16.8 Hz, 9H).
129799-15-1, As the paragraph descriping shows that 129799-15-1 is playing an increasingly important role.
Reference£º
Patent; VIVACE THERAPEUTICS, INC.; LIN, Tracy Tzu-Ling Tang; KONRADI, Andrei W.; VACCA, Joseph; SHEN, Wang; COBURN, Craig; (231 pag.)WO2017/58716; (2017); A1;,
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