Novel method for catalytically synthesizing osimertinib intermediate with a graphene/Pd catalyst

• Main Authors: GAO LINGFENG, ZHENG GENGXIU, CUI ZHAOXIN, GU HAIYANG
• Format: Patent
• Language: Chinese; English
• Published: 02.03.2018
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a novel method for catalytically synthesizing an osimertinib intermediate, [2-[2-dimethylamineethylmethylamine]-4-methoxy-5-benzyloxyamide]phenylamine, with a graphene/Pd catalyst. In the method, an osimertinib intermediate, N-carbobenzoxy-2-methoxy-4-[2-dimethylamineethylmethylamine]-5-nitrophenylamine, is used as a raw material; the nitro group then is reduced into an amino group by hydrogen under light irradiation with the graphene/Pd catalyst, thereby producing the [2-[2-dimethylamineethylmethylamine]-4-methoxy-5-benzyloxyamide]phenylamine, yield being higher than 95% and purity being higher than 98%. Compared with other methods, the method has gentle reaction conditions and is more environment-friendly and has simple operations; the reaction is more high-effective and rapid, and the catalyst has high wear resistance and recycle rate. The intermediate and the final product have high quality; the method has advantages in industrial production. 本发明公开了种石墨烯钯催化剂催化合成奥希替尼中间体［2-［2-二甲胺乙基甲基胺