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Preparation method of dexmethylphenidate

A technology of dextromethylphenidate hydrochloride and methyl phenylacetate, which is applied in the field of preparation of dextromethylphenidate hydrochloride, can solve the problems of long synthesis steps, many wastes, inconvenient industrialization, etc., and save manpower and time costs , Improve production efficiency, low cost effect

Inactive Publication Date: 2019-08-09
南京焕然生物科技有限公司
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Problems solved by technology

Synthetic D-methylphenidate hydrochloride synthetic method at present is as attached figure 2 As shown, there are following problems in this synthetic method: long synthetic steps; low yield; many wastes; high cost, not convenient for industrialization

Method used

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  • Preparation method of dexmethylphenidate
  • Preparation method of dexmethylphenidate

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Experimental program
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Embodiment 1

[0026] A kind of preparation method of D-methylphenidate hydrochloride, is characterized in that, comprises the following steps:

[0027] Step 1: Add 100g of methyl phenylacetate to 1000ml of piperidine, heat up and reflux for 10 hours, and track in the liquid phase. After the reaction was completed, it was concentrated to dryness to obtain 142g of intermediate 1, with a yield of 95%.

[0028] Step 2: Add 142g of the product from the previous step into 500ml of toluene, add 150g of TsN3 in batches, heat up to 70°C and react for 5 hours. After the reaction is completed, the intermediate 2 does not need to be separated, and the reaction solution directly enters the next step of reaction.

[0029] Step 3: Add 0.5g (R)-(-)-[(S)-2-benzhydrylphosphinoferroceneethyl-di-tert-butylphosphonium to the solution in the previous step, heat up to reflux, and after the reaction is complete , cooling and crystallization, filtering, washing the filter cake with toluene, and drying to obtain 1...

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Abstract

The invention relates to a new synthetic route of dexmethylphenidate. Methyl phenylacetate serves as a raw material, and the dexmethylphenidate is synthesized at high yield through four steps of an amidation reaction, a diazotization reaction, a cyclization reaction and a rearrangement reaction. The preparation method of the dexmethylphenidate is high in yield, low in cost, environmentally friendly, easy to operate and suitable for industrialization.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a preparation method of dextromethylphenidate hydrochloride. Background technique [0002] ADHD is a common name for attention deficit and hyperactivity disorder (Attention deficit and hyperactivity disorder, ADHD). A set of syndromes. ADHD is a relatively common disorder in children, and its prevalence rate is generally reported as 3%-5%, and the male-to-female ratio is 4-9:1. According to statistics, there are more than 20 million ADHD patients in my country, and an incomplete statistical report on delinquent juveniles shows that about 75.53% of delinquent juveniles were diagnosed with ADHD during school age. ADHD has become a major illness that seriously threatens the healthy growth of children. [0003] Methylphenidate is currently the most prescribed and most researched ADHD treatment drug. Its mechanism of action is still unclear. Most scholars believe that it mainly promotes th...

Claims

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Application Information

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IPC IPC(8): C07D211/34
CPCC07D211/34
Inventor 王坤鹏韩月林
Owner 南京焕然生物科技有限公司
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