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Preparation of trimethoprim
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A kind of technology of trimethoprim and trimethoxybenzaldehyde, applied in the field of medicine
Inactive Publication Date: 2013-09-18
SHOUGUANG FUKANG PHARMA
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Another research report uses acrylonitrile to replace methoxyacrylonitrile and 3,4,5-trimethoxybenzaldehyde (TMB) condensation, and the yield of its condensation step and subsequent cyclization step does not significantly improve (Chinese Science Journal of Technical University, 31(2) April 2001, pp. 229-234)
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Embodiment 1
[0017] In a 1000mL four-necked flask (equipped with a reflux separator), add 49g (0.25mol) of TMB, 42.5g (0.29mol) of anilinopropionitrile, 150mL of dimethylsulfoxide, 15g of sodium methoxide, and 100mL of toluene, and heat up to 110°C , when the reflux reaction brings water until no water drops are generated in the water separator, stop the reaction, distill toluene under reduced pressure, then add 400mL of water, stir and cool to 5-10°C, filter with suction, and obtain 78.5g of product after drying (yield 97%). mp: 132.5-132.5°C.
[0018] Take 32g of the above-mentioned compound, 19g of guanidine hydrochloride, and 50g of sodium methoxide into a 500mL three-necked flask, add 100mL of ethanol, heat and reflux for 1 hour, evaporate part of the solvent, add 100mL of water, stir and cool down to 5-10°C, filter with suction, and bake TMP27.5g (yield 96%) was obtained after drying. mp: 201.5-201.7°C; HPLC content: 98.7%.
Embodiment 2
[0020] In a 2000mL four-neck flask (equipped with a reflux separator), add TMB98g (0.5mol), anilinopropionitrile 85 (0.58mol)g, dimethylsulfoxide 250mL, sodium methoxide 50g, benzene 300mL, heat up to reflux at 85°C Separate the water until no water drops are formed in the water separator, stop the reaction, recover benzene under reduced pressure, then add 750mL of water, stir and cool down to 5-10°C, filter with suction, and dry to obtain 155g of the product (95.5% yield) . mp: 132.0-132.2°C.
[0021] Take 64g of the above compound, 38g of guanidine hydrochloride, and 100g of sodium methoxide into a 1000mL three-necked flask, add 200mL of ethanol, heat and reflux for 1 hour, evaporate part of the solvent, add 200mL of water, stir and cool down to 5-10°C, and suction filter to obtain the product 56g (96.1% yield). mp: 201.6-201.8°C; HPLC content: 98.8%.
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Abstract
The invention provides a novel intermediate for preparing trimethoprim and a novel method for preparing the trimethoprim by the intermediate. The method of 'dealing with different problems in the same way' is adopted. The operation is convenient, the yield is high, the cost is low and the industrial control is easy to realize.
Description
technical field [0001] The invention relates to a preparation method in the technical field of medicine, in particular to a preparation method of trimethoprim (TMP). Background technique [0002] Trimethoprim (TMP), whose chemical name is 5-[(3,4,5-trimethoxyphenyl)-methyl]-2,4-pyrimidinediamine, is a broad-spectrum high-efficiency and low-toxicity Antimicrobials and fungicides. It has been widely used in the pharmaceutical industry as a fungicide and a fungicide synergist for decades. It not only has excellent synergistic effect in combination with sulfonamide drugs, but also has good synergistic effect on various biological antibiotics and synthetic antibiotics, so it has been widely used in clinical medicine and veterinary animal husbandry, and has become my country's pharmaceutical industry. One of the pillar products. [0003] At present, most industrial manufacturers of TMP use methoxypropionitrile and 3,4,5-trimethoxybenzaldehyde (TMB) to condense to form methyl et...
Claims
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