1-(4-aMino-5-Methoxy-2-Methylphenyl)-N,N-diMethylpiperidin-4-aMine

Uses

1-(4-Amino-3-methoxyphenyl)-N,N-dimethyl-4-piperidinamine is a useful reagent for organic synthesis.

Synthesis

General procedure for the synthesis of 1-(4-amino-3-methoxyphenyl)-N,N-dimethylpiperidin-4-amine from BRIGATINIB intermediates: 4.09 g of Compound 29 was added to a reaction flask and dissolved with 40 mL of methanol. Subsequently, 0.4 g of 10% Pd/C catalyst (based on 10% of the mass of Compound 29) was added for the hydrogenation reduction reaction. The progress of the reaction was monitored by TLC and the reaction was complete after about 6 hours. After stopping the reaction, the reaction mixture was filtered and the catalyst was washed with a small amount of methanol. The filtrate was concentrated by distillation under reduced pressure to give 3.38 g of brown solid product 7-6 in 92.60% yield.

References

[1] Patent: CN106905245, 2017, A. Location in patent: Paragraph 0249; 0259; 0260; 0261; 0262
[2] Patent: KR2016/37844, 2016, A. Location in patent: Paragraph 0304; 0306
[3] Patent: EP3372594, 2018, A1. Location in patent: Paragraph 0126; 0128; 0264; 0265
[4] Patent: US2008/300242, 2008, A1. Location in patent: Page/Page column 86
[5] Patent: WO2010/138575, 2010, A1. Location in patent: Page/Page column 82