Cariprazine tartrate, preparation method therefor and medical use thereof

[0028] Embodiment 1: the preparation of cariprazine tartrate

[0029] Dissolve 30g of cariprazine in 650ml of absolute ethanol, stir and heat to 60-65°C, add 10.5g of tartaric acid, keep stirring for 2h, cool to 0-5°C, let stand for 5h, filter, and use proper amount of absolute ethanol for solid After washing, vacuum drying at 65-70°C for 6 hours, 35.8 g of cariprazine tartrate was obtained, with a yield of 74%, mp: 266-268°C (decomposition). HPLC content 99.2%.

[0030]

[0031] 1 H—NMR (400MHz, CDCl 3 / TMS,ppm):

[0032] δ: 6.91~7.15(m, 3H, Ar- H ), 1.08~1.53(m, 7H, cyclohexane- H ), 2.55~2.62(m, 4H, piperazine-7 H ), 3.11~3.26(m, 4H, piperazine- H ), 1.79~1.82 (m, 2H, -NC H 2 CH 2 -), 2.07~2.12(t, 2H, J=7.6Hz, -NCH 2 C H 2 -), 3.76~3.79(m, 1H, piperazine-1 H ), 6.54~6.57 (m, 1H, N H ), 2.83~2.95(m, 6H, N(C H 3 ) 2 ).

[0033] MS: m / z (M + ) 428 (M-C 4 h 6 o 6 +H).

[0034] Embodiment 2: the preparation of cariprazine hydrochloride

[0035] Dissolve 15g of cariprazine in 150ml of N-methylpyrrolidone, stir and heat to 30-35°C, drop in 12ml of isopropanol solution of 25-35% hydrogen chloride, keep stirring for 1h, then add 300ml of isopropanol, and stir for 10min , cooled to 0-5°C, let stand for 2h, filtered, washed the solid with an appropriate amount of isopropanol, and dried in vacuum at 65-70°C for 6h to obtain 12.3g of cariprazine hydrochloride.

[0036] Embodiment 3: physicochemical property comparison

[0037] According to the four routine tests of the Chinese Pharmacopoeia 2015 edition.

[0038] Conclusion: Cariprazine tartrate of the present invention has good solubility and fluidity, and is not hygroscopic.