1-Methyl-N-(4-nitrophenyl)piperidin-4-amine synthesis

Yield:93591-87-8 85%

Reaction Conditions:

with triethylamine in dimethyl sulfoxide at 90;

Steps:

138 Preparation of N-(3-(2-((4-((l-methylpiperidin-4-yl)amino)phenyl)amino)quinazolin-8-yl)phenyl)acrylamide

To a solution of l-methylpiperidin-4-amine (1.25 g, 11 mmol, 1.1 eq.) in DMSO (20 mL) was added TEA ( 4.2 mL 30 mmol, 3 eq.) followed by l-fluoro-4-nitrobenzene (1.41 g, 10 mmol, 1 eq.) and the mixture was stirred at 90 °C overnight. The mixture was poured into ice-water (40 mL), and the precipitate was collected by filtration, dried in vacum to afford l-methyl-N-(4-nitrophenyl)piperidin-4-amine (2 g, 85%) as a white solid.

References:

WO2015/27222,2015,A2 Location in patent:Paragraph 0415