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 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.
Synthetic method 2 -amino -6 - chloropurine
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Paragraph 0048-0075, (2021/08/25)
The invention provides a synthetic method of 2 - amino -6 - chloropurine, and belongs to the field of organic synthesis. The synthesis method provided by the invention comprises the following steps: adding 2 -acetyl-6-hydroxypurine into the reaction container. The product and comprises hexachloroacetone, organic base A chloride, heating reflux reaction 2h - 48h, distillation to remove dimethyl sulfoxide, adding alkali liquor pH, reacting 1h - 12h, adjusting 7.0 - 7.5 to 2 - and separating and purifying to obtain the amino -6 - chloropurine of the target product. The nitrogen-containing phosphorus-containing reagent is greatly reduced, the emission of nitrogen-containing phosphorus-containing wastewater is reduced correspondingly, and large-scale process production is facilitated.