The invention belongs to the technical field of chemical
medicine raw material medicine and preparation manufacturing, and particularly relates to a preparation method of a
varenicline tartrate intermediate. According to the present invention, 2, 3, 4, 5-tetrahydro-7, 8-dinitro-3-(trifluoroacetyl)-1, 5-
methylene-1H-3-benzaza is adopted as a
raw material, and the 2, 3, 4, 5-tetrahydro-7, 8-diamino-3-(trifluoroacetyl)-1, 5-
methylene-1H-3-benzaza is prepared through the reduction of disulfurous acid or a salt thereof, such that the method does not need to use
hydrogen pressurization, can be used for preparing the 2, 3, 4, 5-tetrahydro-7, 8-diamino-3-(trifluoroacetyl)-1, 5-
methylene-1H-3-benzaza, and can be used for preparing the 2, 3, 4, 5-tetrahydro-7, 8-diamino-3-(trifluoroacetyl)-1, 5- meanwhile, the use of heavy
metal palladium is avoided, the reaction condition is mild, the cost is low, the target product yield is high (greater than 75%), the purity is excellent (greater than 97%), and the industrial production of
varenicline tartrate is facilitated.