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Trifluoperidol is a synthetic compound that is used as a precursor in the production of certain pharmaceuticals and dyes.
The production process of trifluoperidol involves several steps, which are outlined below.
Step 1: Synthesis of 2,3-dimethyl-1,4-benzoxazepine
The first step in the production of trifluoperidol is the synthesis of 2,3-dimethyl-1,4-benzoxazepine, which is synthesized by reaction of dimethyl-1,4-benzoxazepine with chloral hydrate in the presence of an acid catalyst.
Step 2: Condensation of 2,3-dimethyl-1,4-benzoxazepine with acetic anhydride
Next, 2,3-dimethyl-1,4-benzoxazepine is condensed with acetic anhydride in the presence of a strong acid catalyst to form 1-(2,3-dimethyl-1,4-benzoxazepin-7-yl)-3-(acetoxy)-propan-2-one.
Step 3: Reduction of 1-(2,3-dimethyl-1,4-benzoxazepin-7-yl)-3-(acetoxy)-propan-2-one
The next step is the reduction of 1-(2,3-dimethyl-1,4-benzoxazepin-7-yl)-3-(acetoxy)-propan-2-one using a reducing agent such as lithium aluminum hydride (LiAlH4) to form 1-(2,3-dimethyl-1,4-benzoxazepin-7-yl)-3-(hydroxy)-propan-2-one.
Step 4: Bromination of 1-(2,3-dimethyl-1,4-benzoxazepin-7-yl)-3-(hydroxy)-propan-2-one
The bromination of 1-(2,3-dimethyl-1,4-benzoxazepin-7-yl)-3-(hydroxy)-propan-2-one is carried out using a bromine source, such as N-bromosuccinimide (NBS), in the presence of a solvent such as chloroform.
Step 5: Coupling of 4-bromo-1-(2,3-dimethyl-1,4-benzoxazepin-7-yl)-3-hydroxy-propan-2-one with tetracyclic guanidine
The next step is the coupling of 4-bromo-1-(2,3-dimethyl-1,4-benzoxazepin-7-yl)-3-hydroxy-propan-2-one with tetracyclic guanidine to form 1,4-dimethyl-7-[4-(4-bromo-1,3-oxazepan-2-yl)-tetracyclo[4.
4.
0.
12,5.
17,10]hept-9-yl]-1,4-benzoxazepine.
Step 6: Reduction of 1,4-dimethyl-7-[4-(4-bromo-1,3-oxazepan-2-yl)-tetracyclo[4.
4.
0.
12,5.
17,10]hept-9-yl]-1,4-benzoxazepine
The last step is the reduction of 1,4-dimethyl-7-[4-(4-bromo-1,3-oxazepan-2-yl)-tetracyclo[4.
4.
0.
12,5.
17,10]hept-9-yl]-1,4-benzoxazepine using a reducing agent such as lithium aluminum hydride (LiAlH4) to form trifluoperidol.
Overall, the production process of trifluoperidol involves several steps, including the synthesis of