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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[0029] 1. Production raw materials:
[0030] raw material name
Production usage
Specification
D-serine
24kg
98%
12kg
---
387kg
AR
80kg
CP
Phosphorus pentachloride
37.29kg
CP
481kg
CP
11.6kg
99%
Glacial acetic acid
25kg
CP
40kg
CP
Isopropanol
167kg
CP
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
12kg
150kg
80kg
[0035] Specific operation process:
[0036] Add 150kg of anhydrous...
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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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IPC IPC(8): C07D261/04
CPCC07D261/04C07B2200/07
Inventor 周如国刘维坦高彬洁
Owner ANHUI YOUCARE KAIYUE PHARMA

