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The preparation method of deuterated pimozide

A technology of pimozide and deuterium, which is applied in the field of preparation of deuterated pimozide, can solve problems such as undiscovered reports, and achieve the effects of easy purification, reasonable process design, and high yield

Active Publication Date: 2017-05-03
TLC NANJING PHARMA RANDD CO LTD
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AI Technical Summary

Problems solved by technology

[0004] Stable isotope-labeled pimozide-d4 can be well used in clinical pharmacokinetic research, so as to more accurately and conveniently understand the metabolic process and mechanism of action of pimozide in the human body, while stable isotope The synthesis of labeled pimozide-d4 compounds has not been reported yet

Method used

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  • The preparation method of deuterated pimozide
  • The preparation method of deuterated pimozide
  • The preparation method of deuterated pimozide

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Embodiment 1

[0029] like figure 1 The process flow diagram for the preparation of deuterated pimozide.

[0030] The preparation of intermediate 3: get the magnesium powder of 0.43 gram and suspend in 3ml tetrahydrofuran, add the iodine of catalyst amount, the mixture is warmed up to 60 ℃, dropwise the p-fluorobromobenzene (being compound 1) of 3 grams deuterated in 7ml tetrahydrofuran The solution was added dropwise for about 10min. After the dropwise addition, the reaction was heated to 70°C for 1.5 hours to obtain the Grignard reagent of deuterated p-fluorobromobenzene, and then the obtained Grignard reagent was cooled to room temperature, and 2.75 grams of intermediate 2 were added thereto. The tetrahydrofuran solution was reacted at 40°C for 1 hour, then the reaction solution was lowered to room temperature, saturated ammonium chloride aqueous solution was added, extracted with acetic acid, the organic phase was washed with saturated sodium chloride, the organic phase was dried, and th...

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Abstract

The invention discloses a preparation method of deuterated pimozide. The pimozide-d4 is synthesized from 4-bromopentafluorobenzene-d4 through eight steps. The provided preparation method has the advantages of reasonable technological design, simple operation, easy product separation and purification, easily-available raw materials, high yield, and high purity. The isotope abundance of the obtained target product is high. The prepared stable isotope-labeled pimozide-d4 can be well applied to clinical pharmacokinetics researches, so people can acknowledge the metabolism process and action mechanism of pimozide in human body more precisely and conveniently, and thus the deuterated pimozide has an important application value.

Description

technical field [0001] The invention belongs to the technical field of preparation of stable isotope-labeled raw materials, and in particular relates to a preparation method of deuterated pimozide. Background technique [0002] Pimozide (Pimozide), whose drug alias is pimozide, Opiram, Orap was first listed in Belgium in 1970, which belongs to the difluorobenzene derivative of droperidol, and is clinically used for the treatment of schizophrenia, mania and Tourette syndrome. This drug has better anti-hallucination and delusional effects, and it can activate patients who are chronically withdrawn and passive. Has a longer-acting antipsychotic effect. For acute and chronic schizophrenia, it has good effect on hallucinations, delusions and apathy. It is especially suitable for chronic shrinkage patients. Compared with chlorpromazine, its sedative, antihypertensive, anticholinergic and other side effects are weaker. [0003] Stable isotope-labeled drug substances are the sa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/04
CPCC07D401/04
Inventor 储文刘春王忠义
Owner TLC NANJING PHARMA RANDD CO LTD
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