Analyzing the synthesis route of Methyl 1-Boc-piperazine-2-carboxylate

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

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.

To a solution of 7-benzyl-2,4-dichloro-6,8- dihydro-5H-pyrido[3,4-d] pyrimidine (2.00 g, 6.80 mmol, 1.00 eq) in DMSO (40.0 mL) was added DIEA (1.76 g, 13.6 mmol, 2.38 mL, 2.00 eq) and 1-tert-butyl 2-methylpiperazine-l,2- dicarboxylate (1.74 g, 7.14 mmol, 1.05 eq). The mixture was stirred at 55 C for 16 hours. The mixture was diluted with water (100 mL) and extracted with ethyl acetate (3 x 100 mL). The combined organic layers were washed with brine (3 chi 100 mL), dried over Na2S04, filtered and concentrated to dryness. The residue was purified by column chromatography (S1O2, diethyl ether/ethyl acetate = 1 :0 to 3 : 1) to give 1-tert-butyl 2-methyl-4-(7-benzyl-2-chloro-6,8-dihydro- 5H-pyrido[3,4-d]pyrimidin -4-yl)piperazine-l,2-dicarboxylate (3.10 g, 5.70 mmol, 83.8 % yield, 92.3 % purity) as a yellow semisolid. ESI MS m/z 502.2 [M+H]+.

129799-15-1, The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MIRATI THERAPEUTICS, INC.; ARRAY BIOPHARMA, INC.; FISCHER, John, P.; FELL, Jay, Bradford; BLAKE, James, F.; HINKLIN, Ronald, Jay; MEJIA, Macedonio, J.; HICKEN, Erik, James; CHICARELLI, Mark, Joseph; GAUDINO, John, J.; VIGERS, Guy, P.A.; BURGESS, Laurence, E.; MARX, Matthew, Arnold; CHRISTENSEN, James, Gail; LEE, Matthew, Randolf; SAVECHENKOV, Pavel; ZECCA, Henry, J.; (529 pag.)WO2017/201161; (2017); A1;,
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