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Preparation method for nefopam hydrochloride

A technique for preparing Nefopam hydrochloride and its preparation steps, which is applied in the field of preparation of Nefopam hydrochloride, and can solve problems such as complex reaction steps and difficult implementation

Pending Publication Date: 2018-01-09
KAMP PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Existing synthetic route has following shortcoming: reaction step is complicated, is difficult for implementing

Method used

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  • Preparation method for nefopam hydrochloride
  • Preparation method for nefopam hydrochloride
  • Preparation method for nefopam hydrochloride

Examples

Experimental program
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Embodiment

[0027] (1) For the preparation route of the intermediate N-(2-(benzoyl)benzyl)-N-methyl-carbamate tert-butyl ester, see figure 2 :

[0028] Add the raw material N-benzyl-N-methylcarbamate tert-butyl ester (22.1g, 0.1mol) and diethyl ether (100mL) into the nitrogen protection reaction system, cool down to -78°C, and slowly add n-butyllithium dropwise (44mL, 2.5M), add phenylacetyl chloride (16.7g, 0.12mol) diethyl ether solution (50mL) dropwise after 30 minutes of reaction, and react at this temperature for 1 hour after addition, then rise to room temperature, add water and stir for several minutes , separate layers, wash the organic layer with water, dry, and distill under reduced pressure to obtain 22.6 g of intermediate (2), with a yield of 70%.

[0029] (2) For the preparation route of intermediate 1-((2-(methylamino)methyl)phenyl)-1-phenylmethanol hydrochloride see image 3 :

[0030] The intermediate N-benzyl-N-methylcarbamate tert-butyl ester (22.0g, 0.07mol), methan...

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Abstract

The invention discloses a preparation method for nefopam hydrochloride. The preparation method is characterized by comprising the following preparation steps: (A) performing a reaction on raw materials including tert-butyl N-benzyl-N-methyl carbamate and benzoyl chloride to obtain an intermediate tert-butyl N-(2-(benzoyl)benzyl)-N-methyl carbamate; (B) performing reduction on the intermediate tert-butyl N-(2-(benzoyl)benzyl)-N-methyl carbamate by a reductant, and performing acidolysis to obtain an intermediate 1-((2-(methylamino)methyl)phenyl)-1-phenylmethanol hydrochloride; and (C) performinga reaction on the intermediate 1-((2-(methylamino)methyl)phenyl)-1-phenylmethanol hydrochloride and chloroacetyl chloride to form an amide through a one-pot method, performing cyclization, and performing reduction by a reductant to obtain the objective compound nefopam hydrochloride. According to the invention, the reaction steps are simple, and the preparation method is easy to implement.

Description

technical field [0001] The invention belongs to the field of chemical medicine synthesis, and in particular relates to a preparation method of Nefopam hydrochloride. Background technique [0002] Nefopam hydrochloride, chemical name 5-methyl-1-phenylpropyl-3,4,5,6-tetrahydro-1H-2,5-oxazapine hydrochloride, is a new type, Non-narcotic, non-morphine receptor agonist analgesic, which does not have the characteristics of non-steroidal anti-inflammatory drugs, it can increase the pain threshold, its effect is not blocked by naloxone, and its analgesic effect is stronger than that of Morphine and aspirin have a slow onset but a longer duration of action, without tolerance and addiction. In addition, it has antipyretic, local anesthetic and anti-inflammatory effects, can slow down the increase of capillary permeability in the early stage of inflammation, and has inhibitory effects on inflammatory edema, exudation and granulation tissue hyperplasia caused by inflammation and prolif...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D267/22
Inventor 张春盛刘达吴健民张静
Owner KAMP PHARMA
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