- 2,4,6-Trichloropyrimidine. Reaction with sodium amide
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The first reaction between 2,4,6-trichloropyrimidine 1 and anionic nitrogen nucleophiles is described. Treatment of 1 with one equivalent of sodium amide gave mixtures of 4-amino-2,6-dichloropyrimidine 2 and 2-amino- 4,6-dichloropyrimidine 3. Additional quantities of sodium amide failed to provide either diamino- or triaminopyrimidines. Instead, the strongly basic nature of sodium amide led to higher molecular products that were not characterized.
- Delia, Thomas J.,Meltsner, Bernard R.,Schomaker, Jennifer M.
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- Large-scale solvent-free chlorination of hydroxy-pyrimidines,-pyridines,- pyrazines and-amides using equimolar POCl3
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Chlorination with equimolar POCl3 can be efficiently achieved not only for hydroxypyrimidines, but also for many other substrates such as 2-hydroxy-pyridines,-quinoxalines, or even-amides. The procedure is solvent-free and involves heating in a sealed reactor at high temperatures using one equivalent of pyridine as base. It is suitable for large scale (multigram) batch preparations.
- Wang, Han,Wen, Kun,Wang, Le,Xiang, Ye,Xu, Xiaocheng,Shen, Yongjia,Sun, Zhihua
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- Synthesis method of 4-amino-2,6-dimethoxyl pyrimidine
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The invention discloses a synthesis method of 4-amino-2,6-dimethoxyl pyrimidine, and belongs to the technical field of medical technologies. The synthesis method comprises following steps: (1) aminolysis reaction: adding 4,6-dichloropyrimdine-5-formic acid into ammonia liquor to carry out aminolysis reactions to obtain 4-amino-6-chloropyrimdine-5-formic acid; (2) chlorination reaction: dissolving4-amino-6-chloropyrimdine-5-formic acid prepared in the step (1) in a water solution of a diluted acid, then adding a chlorination reagent, and carrying out chlorination reactions to obtain 4-amino-2,6-chloropyrimdine-5-formic acid; (3) decarboxylation reaction: in a solvent, carrying out high temperature decarboxylation of 4-amino-2,6-chloropyrimdine-5-formic acid prepared in the step (2) to obtain 4-amino-2,6-chloropyrimdine; and (4) methoxylation reaction: adding 4-amino-2,6-chloropyrimdine prepared in the step (3) into a methoxylation reagent, and carrying out methoxylation reactions to obtain 4-amino-2,6-dimethoxyl pyrimidine. The synthesis method adopts a novel synthesis route, which will not generate a large amount of phosphorus containing wastewater. The provided method is green and environmentally friendly and generates prominent social benefits.
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Paragraph 0030; 0034; 0036; 0040; 0042; 0046; 0048; 0052
(2020/05/01)
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