Production technology of cycloserine

A technology of cycloserine and production process, applied in the field of production technology of cycloserine, can solve the problems of long steps and high synthesis cost, and achieve the effects of low cost, stable yield and controllable quality

Inactive Publication Date: 2016-06-08
ANHUI YOUCARE KAIYUE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] It can be seen from the above route that the steps of this route are long and need to be split, and the synthesis cost is relatively high

Method used

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  • Production technology of cycloserine
  • Production technology of cycloserine
  • Production technology of cycloserine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0029] 1. Production raw materials:

[0030] raw material name

Production usage

Specification

D-serine

24kg

98％

hydrogen chloride

12kg

---

Anhydrous Methanol

387kg

AR

ethyl acetate

80kg

CP

Phosphorus pentachloride

37.29kg

CP

Dichloromethane

481kg

CP

Hydroxylamine hydrochloride

11.6kg

99％

Glacial acetic acid

25kg

CP

sodium hydroxide

40kg

CP

Isopropanol

167kg

CP

activated carbon

3.5kg

Medicinal

Absolute ethanol

31.5kg

AR

[0031] 2. Production process

[0032] (1) Preparation of D-serine methyl ester hydrochloride

[0033] Feeding:

[0034] Material name

Dosage

D-serine

24kg

hydrogen chloride

12kg

Anhydrous Methanol

150kg

ethyl acetate

80kg

[0035] Specific operation process:

[0036] Add 150kg of anhydrous...

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PUM

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Abstract

The invention belongs to the field of chemical synthesis, and particularly relates to a production technology of cycloserine. According to the synthesis technology, D-serine is used as a starting material, three reactions of esterification, chlorination and cyclization are performed, and the cycloserine is obtained. The technological process is simple, the yield is high, and the purity is high. During the esterification reaction, diethyl ether is replaced with ethyl acetate, no 8-hydroxyquinoline is added for crude product preparation after the cyclization reaction, and usage of reagent diethyl ether likely to produce toxicity and the dangerous product 8-hydroxyquinoline is avoided. Meanwhile, the synthesis route is short, the cost is low, and the obtained product is stable in yield and controllable in quality.

Description

technical field [0001] The invention belongs to the field of chemical synthesis, and in particular relates to a production process of cycloserine. Background technique [0002] Cycloserine, also known as D-4-amino-3-isoxazolidinone, is an antibiotic drug that has a good inhibitory effect on Mycobacterium tuberculosis. Because bacteria are not easy to develop drug resistance to it, it is mainly used clinically to treat the infection of drug-resistant Mycobacterium tuberculosis. In addition, studies have found that cycloserine is a special regulator of excitatory amino acid NMDA (N-methyl-D-aspartate) receptors in the central nervous system, and it is also effective in the treatment of psychological diseases such as psychological phobia, depression, and schizophrenia. It has good auxiliary curative effect, and it is also an important intermediate in the synthesis of atypical β-lactam antibiotic Lactivicin. Therefore, cycloserine has broad application prospects and huge marke...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D261/04
CPCC07D261/04C07B2200/07
Inventor 周如国刘维坦高彬洁
Owner ANHUI YOUCARE KAIYUE PHARMA
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