| abstract |
The present invention comprises the steps of reacting the acrylonitrile and the tetrafluoroborate salt of the diazonium ions of 2,6-dimethyl-4-amino-1-carboxybenzyl phenylamine (VI) in the presence of palladium acetate, followed by acid Treatment and subsequent conversion to a hydrochloride (II) thereof with an undesirable Z isomer of less than 0.5%, the core Rilpvirine intermediate, ie (E) -4- (2-cyanoethenyl) The present invention relates to the preparation of -2,6-dimethylphenylamine hydrochloride (II), which provides rilpivirine hydrochloride having a Z-isomer of less than 0.1%. |