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 stirred solution of piperazine-1, 2-dicarboxylic acid 1-teit-butyl ester2-methyl ester (977 mg, 4.0 mmol) in DCM (20 mL) at 0 00 was added4-bromo-benzenesulfonyl chloride (1.02 mg, 4.0 mmol). Then TEA (404 mg, 4.0mmol) was added dropwise and the mixture was stirred at room temperature for 1hr. The mixture was concentrated and purified by silica gel chromatography(petroleum ether/EtOAc = 20/1 to 5/1) to afford 1.66 g (90%) of the titlecompound as a white solid. 1H NMR (400 MHz, ODd3) O [ppm] 7.69 (d, J = 8.8Hz, 2H), 7.61 (d, J= 8.8 Hz, 2H), 4.89-4.60 (m, 1H), 4.27-4.20 (m, 1H), 4.04-3.82(m, 1H), 3.77 (5, 3H), 3.76-3.61 (m, 1H), 3.35-3.11 (m, 1H), 2.51 (dd, J= 11.6, 4.0Hz, 1H), 2.33 (td, J= 11.6, 4.0 Hz, 1H), 1.44 (5, 9H).
The synthetic route of 129799-15-1 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; PFIZER INC.; ITEOS THERAPEUTICS; NINKOVIC, Sacha; CROSIGNANI, Stefano; SCALES, Stephanie Anne; MCALPINE, Indrawan James; COLLINS, Michael Raymond; MADERNA, Andreas; WYTHES, Martin; (295 pag.)WO2016/147144; (2016); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics