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.
Synthesis method of 2-amino-6-chloroguanine
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Paragraph 0052-0057, (2021/08/11)
The invention provides a synthesis method of 2-amino-6-chloroguanine, the synthesis method comprises the following steps: synthesizing 2-amino-6-chloroguanine; according to the method disclosed by the invention, a route of a 2, 4, 5-triamino-6-chloropyrimidine intermediate is not adopted, but 4-chloro-5, 6-dinitropyrimidine-2-amine is taken as an intermediate, and 2-amino-6-chloroguanine is obtained by cyclization on the basis of the intermediate. The synthesis method has few steps, each step is easy to carry out, and the product is high in yield and high in purity, so that the total yield of the 2-amino-6-chloroguanine is relatively high; the method is suitable for industrial production of the 2-amino-6-chloroguanine, and has a wide commercial prospect.
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.