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A technology of diacetyl acyclovir and a synthesis process, applied in the field of organic synthesis, can solve the problems affecting the product yield stability and product quality, the synthesis process is difficult to industrialize production, and the product separation and purification is difficult, etc. The effect of purification and less three wastes
Inactive Publication Date: 2014-03-26
XINXIANG WEIDE CHEM CO LTD
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[0005]2) Using 2,6,9 silanized guanine as raw material, and 2-oxa-1,4-butanediol diethyl ester (OBDDA ), under the catalysis of iodine and phosphate, it condenses into a 9-position substituted product, and then hydrolyzes the product with a yield of 35%, which is relatively low
[0006]3) Using guanine as a raw material, first undergo acetylation to generate N2, N9-diacetyl Guanine (DAG), and then condensed with 2-oxa-1,4-butanediol diethyl ester to generate diacetyl acyclovir (DACV), and then hydrolyzed to obtain the target product, but the 7-position will be generated during the condensation process Diacetyl acyclovir (7-DACV), increases the difficulty of product purification, affects the stability of product yield and product quality
[0008] Although the production process of acyclovir is becoming more and more mature, it is a pity that the following problems generally exist in the existing process: expensive raw materials, use of toxic reagents, reaction Strict conditions, low product quality, low yield, difficult product separation and purification, etc.
The above drawbacks make the synthetic technique of acyclovir bulk drug difficult to suitability for suitability for industrialized production
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Embodiment 1
[0023] a) Synthesis of diacetylguanine
[0024] Add guanosine, acetic anhydride, and boric acid into the reaction kettle at a weight ratio of 1:6.4:0.006, raise the temperature to 110°C-120°C, and keep the temperature for 6 hours. Then the temperature was lowered to 100° C. for 6 hours and the reaction was completed. Part of the reaction solution (40% of the feed amount) was distilled off under reduced pressure. Lower the temperature to 5°C and keep it for 5 hours, discharge and centrifuge, wash with acetic anhydride three times, and dry to obtain diacetylguanine. 1 H NMR (400 MHz,
[0027] Put toluene, diacetylguanine, and aluminum trichloride catalysts into the reaction kettle in proportion, slowly raise the temperature to reflux, separate water, add 2-oxa-...
Embodiment 2
[0031] b) The catalyst used is anhydrous zinc chloride and benzenesulfonic acid, and the weight ratio of the two is 1:2. Others are the same as the above-mentioned embodiment. Obtained content greater than 99.5% acyclovir bulk drug.
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Abstract
The invention discloses a preparation method of acyclovir, and belongs to the field of organic compound synthesis. According to the method, guanosine is taken as a starting raw material and is subjected to reactions of acylation, condensation and hydrolysis to prepare the acyclovir. Compared with the prior art, the synthesis method has stable and abundant raw material sources, market fluctuation influences are small, reaction conditions are mild, the operation is simple and safe, the reaction yield is high, the production cost is low, three wastes are few, and greater implementation value and socioeconomic benefits are provided.
Description
technical field [0001] The invention relates to a synthesis process of acyclovir, which belongs to the field of organic synthesis. Background technique [0002] Acyclovir (ACV), also known as acyclovir, English name acyclovir, chemical name 9-[(2-hydroxyethoxy)methyl]-guanine, is an efficient broad-spectrum antiviral drug , which was first synthesized and applied in the UK in 1981, has now been included in my country's national basic therapeutic drugs, and has a large market demand. The drug is highly effective against type I and type II herpes simplex and varicella zoster virus. With the deepening of people's research, this type of drug can also be applied to anti-HIV virus. [0003] The research on the synthetic method and production process of acyclovir has always been paid attention to by people, and there are multiple synthetic methods so far: [0004] 1) Using 2-chloro-6-iodopurine as raw material, first condense with trimethylsiloxyethyl iodomethyl ether to generate ...
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