(2-Aminophenyl)dimethylphosphine Oxide

(2-Aminophenyl)dimethylphosphine Oxide is mainly used as a raw material or reagent for organic synthesis and can be used to prepare other compounds such as phosphine oxide derivatives and pyrimidine derivatives.

(2-Aminophenyl)dimethylphosphine Oxide is prepared by the reaction of 2-Iodoaniline and Dimethylphosphine oxide. The specific synthesis steps are as follows:
To a solution of 2-iodoaniline ( 1.0 eq) and dimethylphosphine oxide (1.1 eq) in DMF were added potassium phosphate ( 1.1 eq) and palladium acetate/Xantphos (catalytic). The reaction was stirred at 150 °C for 3 hours and cooled to room temperature. The solvent was evaporated and the residue was worked up with DCM/water. The crude product was purified with a column(EtOAc/MeOH 10: 1 ) to give 1 as a brown solid (80percent yield).

[1] Patent: WO2012/151561, 2012, A1. Location in patent: Page/Page column 37
[2] Patent: WO2013/169401, 2013, A1. Location in patent: Page/Page column 41-42
[3] Patent: US2015/225436, 2015, A1. Location in patent: Paragraph 0791-0792
[4] Patent: CN106928275, 2017, A. Location in patent: Paragraph 0097-0099
[5] Journal of Medicinal Chemistry, 2016, vol. 59, # 10, p. 4948 - 4964