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Synthesis method of nimustine hydrochloride

A technology of nimustine hydrochloride and a synthesis method, which is applied in the field of drug synthesis, can solve the problems of hidden danger of operator's personal safety, inability to accurately calculate yield, and high operational risk, and achieves avoiding side reactions, reducing reaction toxicity, The effect of improving safety

Pending Publication Date: 2021-08-24
HAINAN GENERAL & KANGLI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] However, the reagents used in this method are highly toxic and dangerous to operate, which poses a greater safety hazard to the personal safety of operators, and the reaction yield is low, and some steps cannot accurately calculate the yield. The total yield is 56.8%
[0008] Among many anticancer drugs with high cost, nimustine is a chemotherapeutic drug whose raw material is easy to obtain and cheap, and can be tolerated by most people. Due to the problems of large reagents and low accuracy of yield calculation, it is necessary to provide a synthetic method with high safety, no harm to operators and high accuracy of yield detection and calculation

Method used

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  • Synthesis method of nimustine hydrochloride
  • Synthesis method of nimustine hydrochloride
  • Synthesis method of nimustine hydrochloride

Examples

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Embodiment 1

[0026] Embodiment 1 A kind of synthetic method of nimustine hydrochloride A1

[0027] The present embodiment provides a kind of synthetic method of nimustine hydrochloride A1, and its synthetic method is as follows:

[0028] 1) Weigh 79.53g of 2-chloroethylamine and 76.05g of methyl bicarbonate into 300ml of methanol, mix and stir under the protection of nitrogen, after stirring evenly, raise the temperature to 80°C and keep it warm for 1h, take a small amount of reaction solution after 1h , injected into the liquid chromatograph after dilution and carried out routine condition analysis, monitoring the progress of the reaction, the molecular weight appearing in the obtained spectrogram is 122.54 (M - ), and the absorption peak of 2-chloroethylamine disappeared, that is, the end of the reaction was reached. After the reaction, the reaction solution was down to room temperature, concentrated under reduced pressure to dryness, and obtained 101.3g of compound (3), Yield: 82%;

...

Embodiment 2～5

[0035] Embodiment 2~5 a kind of synthetic method of nimustine hydrochloride A2~A5

[0036] The synthetic method of the nimustine hydrochloride A2~A5 that embodiment 2~5 provides, their synthetic method and the synthetic method of the nimustine hydrochloride provided in the embodiment 1 are basically the same, the difference is only different in some process parameters, The specific process parameters are shown in Table 1.

[0037] Table 1: Process parameter list of nimustine hydrochloride A2~A5

[0038]

[0039]

[0040] *: The concentration of dilute nitric acid is 68%; the concentration of hydrochloric acid is 36%.

[0041] Other parameters are all the same as in Example 1.

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Abstract

The invention belongs to the field of medicine synthesis, and discloses a synthesis method of nimustine hydrochloride. According to the synthesis method provided by the invention, 2-chloroethylamine is used as a raw material, and nimustine hydrochloride is obtained after amine ester exchange, condensation reaction and nitration reaction. According to the synthesis method of nimustine hydrochloride provided by the invention, the toxicity of a reaction reagent is reduced, the safety of a synthesis process is improved, and the calculation accuracy of the reaction yield is improved. The invention also provides an application of the synthesis method of the nimustine hydrochloride, the provided synthesis method is suitable for synthesizing the nimustine hydrochloride, and the synthesized nimustine hydrochloride is used for preparing the nimustine hydrochloride for injection.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and relates to a synthesis method of antitumor drugs, in particular to a synthesis method of nimustine hydrochloride. Background technique [0002] Nimustine hydrochloride, chemical name: 1-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-3-(2-chloroethyl)-3-nitroso Urea hydrochloride, CAS number: 55661-38-6, molecular formula: C9H13ClN6O2·HCl, molecular weight: 309.15. [0003] Nimustine hydrochloride can alleviate the subjective symptoms and signs of brain and neck cancer, brain tumor, lung cancer, digestive tract cancer (stomach cancer, colon / rectal cancer, esophageal cancer), malignant lymphoma and leukemia. [0004] At present, malignant tumors rank first in the cause of death among residents in my country, and the incidence of malignant tumors is still on the rise, seriously endangering the lives of patients. Nimustine hydrochloride is an alkylating agent of nitrosoureas. It was first listed in Japa...

Claims

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Application Information

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IPC IPC(8): C07D239/42
CPCC07D239/42
Inventor 符永红林方育肖汉文唐雄肇
Owner HAINAN GENERAL & KANGLI PHARMA
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