10310-21-1Relevant articles and documents
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Balsinger,Montgomery
, p. 1573 (1960)
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A new method to synthesize famciclovir
Luo, Lei,Chen, Guorong,Li, Yuanchao
, p. 2803 - 2808 (2008)
A new and efficient method has been reported for the synthesis of 2-amino-9-[4-acetoxy-3-(acetoxymethyl)butyl-1-yl]purine(famciclovir)starting from guanine. The route involves chlorination of guanine, optimized Mitsunobu reaction, coupling with diethyl malonate, hydrogenation, reduction and esterification,and the overall yield is about 29%. This method does not require any form of chromatographic purification to give pure famciclovir, and it is an industrially viable manufacturing process for this drug. The Japan Institute of Heterocyclic Chemistry.
Preparation methods for 2-amino-6-chloroguanine and intermediates of 2-amino-6-chloroguanine
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Paragraph 0055; 0067; 0070-0071; 0075; 0078-0079, (2021/08/25)
The invention provides preparation methods for 2-amino-6-chloroguanine and intermediates of the 2-amino-6-chloroguanine. The preparation method of the intermediates comprises the following steps: dissolving 2,4-diamino-5-nitroso-6-hydroxypyrimidine in a solvent A and N,N-dimethylformamide, conducting heating for refluxing, dropwise adding a triphosgene solution, carrying out a heat-preserved reaction, and after the reaction is finished, carrying out post-treatment to obtain an intermediate compound II of 2-amino-6-chloroguanine; and then, conducting further treatment to obtain intermediates III to IV and 2-amino-6-chloroguanine. According to the preparation methods of the 2-amino-6-chloroguanine and the intermediates of the 2-amino-6-chloroguanine, a synthesis method of the 2-amino-6-chloroguanine is adopted, so a process of carrying out a chlorination reaction on guanine, which is more expensive and serves as an initial raw material, and phosphorus oxychloride in the prior art is avoided, and meanwhile, the generation of a large amount of high-phosphorus and high-ammonia-nitrogen wastewater which is difficult to treat in the traditional process is avoided.
Preparation method of purine nucleotide intermediate
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Paragraph 0028-0032; 0037-0041; 0046-0050, (2021/06/21)
The invention relates to the technical field of medical intermediates, particularly to a preparation method of a purine nucleotide intermediate. The synthesis route of the preparation method comprises steps as follows: 1) carrying out a chlorination reaction on a raw material compound V and a thionyl chloride/hydrogen peroxide reaction system to obtain a compound IV; 2) reacting the compound IV with methylamine to obtain a compound III; and 3) reacting the compound III with a compound II in the presence of a catalyst to obtain a compound I. According to the invention, the synthetic route of the purine nucleotide intermediate is improved, the methylation is firstly carried out, and then the deprotection is carried out, so that the reaction condition is mild, the operation is simple, the yield and the purity are higher, and the method is suitable for industrial large-scale production.