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The dihydrotetrabenazine (DTBZ) was synthesized by reduction of tetrabenazine with sodium borohydride in ethanol. Crystals suitable for X-ray analysis were obtained from a mixed solution of dichloromethane and ethanol in a five-to-one volume ratio. The crystal is monoclinic, space group P21/c with crystallographic parameters: a = 15.0129(14) , b = 12.5677(12) , c = 9.7715(9) , β = 98.556(2)°, μ = 0.078 mm−1, V = 1823.1(3) 3, Z = 4, Dc = 1.164 g/cm3, F(000) = 696, T = 296(2) K. The X-ray analysis and the chiral HPLC show that the DTBZ prepared by our method consists of (2R,3R,11bR) and (2S,3S,11bS) enantiomers.

The title compound tetrabenazine was synthesized by reaction of 3-dimethyl-aminomethylheptan-2-one and 6,7-dimethoxy-3,4-dihydroisoquinoline hydrochloride. This approach provides an efficient and concise way to the synthesis of the marketed drug tetrabenazine. The colorless single crystal of tetrabenazine suitable for X-ray analysis was obtained from saturated methanol solution. The X-ray results showed that tetrabenazine consists of (3R, 11bR) and (3S, 11bS) enantiomers. Two terminal methyl groups are disordered in the (3R, 11bR) enantiomer.

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