With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5464-12-0,1-(2-Hydroxyethyl)-4-methylpiperazine,as a common compound, the synthetic route is as follows.
10.0 g 2-chloro-3 -methyl-4-(4,4, 5,5 -tetramethyl- 1,3 ,2-dioxaborolan-2-yl)phenol(Preparation 5a) (37.2 mmol), 8.7 g 2-(4-methylpiperazin-1-yl)ethanol (60.3 mmol) and15.8 g PPh3 (60.3 mrnol) were dissolved in 100 mL dry toluene and then 27 mL diethylazodicarboxylate (60.3 mmol, 40percent solution in toluene) was added dropwise. The mixturewas stirred at 50°C under argon for 1.5 hours. The volatiles were evaporated under reducedpressure and 100 rnL Et20 was added. The precipitated white crystals were filtered off and washed with Et20. The filtrate was concentrated under reduced pressure and pudfied via flash chromatography using CHC13 and MeOH as eluents. The resulting light brown oil was crystallized from hexanc to give Preparation Sb as an off-white solid.?11 NMR (500 MHz, DMSO-d6): 7.56 (d, 111), 6.99 (d, 1H), 4.15 (t, 2H), 2.72 (t, 2H), 2.51 (s, 311), 2.50 (br s, 4H), 2.29 (br s, 411), 2.13 (s, 311), 1.29 (s, 12H)., 5464-12-0
The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; KOTSCHY, Andras; SZLAVIK, Zoltan; CSEKEI, Marton; PACZAL, Attila; SZABO, Zoltan; SIPOS, Szabolcs; RADICS, Gabor; PROSZENYAK, Agnes; BALINT, Balazs; BRUNO, Alain; GENESTE, Olivier; DAVIDSON, James Edward Paul; MURRAY, James Brooke; CHEN, I-Jen; PERRON-SIERRA, Francoise; WO2015/97123; (2015); A1;,
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