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.
300 mg mixture of 2,6-dichloro-4- [4-chloro-6-(4-fluorophenyl)thieno [2,3 -d]pyrimidin-5 -yl] -3,5 -dimethyl-pheno 1 and 4- [4-bromo-6-(4-fluorophenyl)thieno [2,3 -d]pyrimidin-5 -yl] -2,6-dichloro-3 ,5 -dimethyl-pheno 1 (0.62 mmo 1), 286 mg 2-(4-methylpiperazin- 1 -yl)ethano 1(1.98 mmol) and 520 mg triphenyl phosphine (1.98 mmol) were dissolved in 10 mL drytoluene, then 460 mg ditertbutyl azodicarboxylate (1.98 mmol) was added. The mixturewas stirred at 50 ¡ãC under nitrogen until no further conversion was observed. The volatiles were evaporated under reduced pressure and the crude intermediate was purified via flash chromatography using EtOAc and methanol as eluents to obtain 4-chloro-5-[3,5-dichloro- 2,6-dimethyl-4- [2-(4-methylpiperazin- 1 -yl)ethoxy]phenyl] -6-(4-fluorophenyl)thieno [2,3 -d]pyrimidine and 4-bromo-5 -[3 ,5-dichloro-2,6-dimethyl-4- [2-(4-methylpiperazin- 1-yl)ethoxy]phenyl]-6-(4-fluorophenyl)thieno[2,3-d]pyrimidine as a 35:65 mixture of products.
5464-12-0, The synthetic route of 5464-12-0 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; LES LABORATOIRES SERVIER; VERNALIS (R&D) LIMITED; SZLAVIK, Zoltan; SZABO, Zoltan; CSEKEI, Marton; PACZAL, Attila; KOTSCHY, Andras; BRUNO, Alain; GENESTE, Olivier; CHEN, I-Jen; DAVIDSON, James Edward Paul; MURRAY, James Brooke; ONDI, Levente; RADICS, Gabor; SIPOS, Szabolcs; PROSZENYAK, Agnes; PERRON-SIERRA, Francoise; BALINT, Balazs; (188 pag.)WO2016/207226; (2016); A1;,
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