106877-20-7

General procedure for the synthesis of 3-methoxy-4-(trifluoromethyl)aniline from 2-methoxy-4-nitro-1-(trifluoromethyl)benzene: Intermediate 444 (7.1 g, 28.9 mmol) was dissolved in methanol (100 mL) followed by addition of 5% Pd/C catalyst (0.7 g). The reaction mixture was hydrogenated under hydrogen atmosphere (50 Psi) for 48 hours at room temperature. Upon completion of the reaction, the catalyst was removed by filtration and the filtrate was concentrated under reduced pressure to give Intermediate 445 (7 g) as a white solid.

[1] Journal of Medicinal Chemistry, 2014, vol. 57, # 5, p. 1914 - 1931
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[3] Patent: WO2017/32840, 2017, A1. Location in patent: Page/Page column 226