The invention discloses a method for synthesizing (1R, 2S)-2, 6-dimethyl-1H-
indene-1-amine, which comprises the following steps: step 1, carrying out
condensation reaction on substituted propionyl
benzene and carbonic ester, and then carrying out ammonification reaction and amidation reaction to generate an
enamine intermediate; 2, in the presence of a
rhodium catalyst and a
chiral ligand, carrying out
asymmetric hydrogenation double bond on the
enamine intermediate obtained in the step 1 to obtain 2-methyl-3-amino-ester; 3, 2-methyl-3-amino-ester obtained in the step 2 is subjected to a cyclization reaction under the
catalysis of acid, and indanone is obtained; 4, performing
catalytic hydrogenation on the indanone obtained in the step 3 by adopting a
palladium catalyst, removing keto carbonyl and positioning
halogen substituent; and step 5, carrying out
hydrolysis on the product obtained in the step 4 to remove the
protecting group so as to obtain the target product (1R, 2S)-2, 6-dimethyl-1H-
indene-1-amine. According to the invention, chiral control of a cyclic trans-
substituent, which is difficult to realize by a conventional method, is ingeniously converted into central control of conventional chain double bonds, and finally, the target central
chirality is obtained by cyclization.