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The present invention provides a method ...
The invention discloses a preparation me...
The invention provides a cariprazine syn...
![3-(trans-4-{2-[4-(2,3-dichlorophenyl)piperazin-1-yl]-2-oxo-ethyl}cyclohexyl)-1,1-dimethylurea](/upload/2025/12/33468fe0-2d65-46b4-b30c-8fb30b5b5655.png)
3-(trans-4-{2-[4-(2,3-dichlorophenyl)piperazin-1-yl]-2-oxo-ethyl}cyclohexyl)-1,1-dimethylurea
Cariprazine
| Conditions | Yield |
|---|---|
|
With
sodium tetrahydroborate; boron trifluoride diethyl etherate;
In
tetrahydrofuran;
at 20 ℃;
for 16h;
Temperature;
Reagent/catalyst;
|
93% |
|
With
lithium aluminium tetrahydride;
In
tetrahydrofuran;
at 0 - 50 ℃;
for 5h;
Reagent/catalyst;
Solvent;
Temperature;
|
91.7% |
|
With
lithium aluminium tetrahydride;
In
acetonitrile;
|
90% |
|
With
sodium tetrahydroborate; boron trifluoride;
In
tetrahydrofuran;
at 0 - 55 ℃;
for 1h;
|
86.2% |
|
With
sodium tetrahydroborate; boron trifluoride diethyl etherate;
In
tetrahydrofuran;
at -20 - 30 ℃;
for 1.75h;
|
13.2 g |
trans-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexane-1-amine
N,N-Dimethylcarbamoyl chloride
Cariprazine
| Conditions | Yield |
|---|---|
|
N,N-Dimethylcarbamoyl chloride;
With
tetrabutyl phosphonium bromide; sodium hydroxide;
In
dichloromethane;
at 50 ℃;
for 1h;
trans-4-(2-(4-(2,3-dichlorophenyl)piperazin-1-yl)ethyl)cyclohexane-1-amine;
In
dichloromethane;
for 50h;
Reagent/catalyst;
Solvent;
Temperature;
|
95% |
|
With
sodium carbonate; sodium hydroxide;
In
dichloromethane;
at 15 - 25 ℃;
for 13h;
Reagent/catalyst;
Solvent;
Temperature;
|
92.1% |
|
With
N-ethyl-N,N-diisopropylamine;
In
dichloromethane;
at 0 - 20 ℃;
for 12h;
Inert atmosphere;
|
63.8% |
|
In
dichloromethane;
at 20 ℃;
for 18h;
|
56% |
|
With
triethylamine;
In
dichloromethane;
|
43% |
bis(trichloromethyl) carbonate
dimethyl amine
trans N-(4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-ethyl}-cyclohexyl)carbamic acid methylester
trans 2-{1-[4-(N-(tert-butoxycarbonyl))amino]cyclohexyl}ethyl acetate
Cariprazine hydrochloride
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