1886-34-6Relevant articles and documents
Synthesis method of formyl pyrimidine
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Paragraph 0108-0127, (2020/07/03)
The invention discloses a synthesis method of formyl pyrimidine, which comprises the following steps: (1) by using formamide and acrylonitrile as raw materials, carrying out Michael addition reactionunder the action of a catalyst A and post-treatment to obtain 3-formamide propionitrile; (2) by taking 3-formamido propionitrile and paraformaldehyde as raw materials, carrying out condensation reaction in the presence of a catalyst B and a benzene solvent, and carrying out post-treatment to obtain N-(2-cyanovinyl)-formamide; and (3) with N-(2-cyanovinyl)-formamide and free acetamidine as raw materials, carrying out a condensation reaction in a low-grade fatty alcohol solvent, then heating, carrying out oxidative aromatization under the action of a catalyst C, and finally, carrying out post-treatment to obtain formyl pyrimidine. The synthesis method disclosed by the invention has the advantages that the route is green, safe and environment-friendly; and an activating group and a leaving group are not adopted, so that the atom economy of the reaction is high.
Synthetic method of 2-methyl-4-amino-5-formyl aminomethylpyrimidine
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Paragraph 0021; 0038, (2019/03/12)
The invention relates to a synthetic method of 2-methyl-4-amino-5-formyl aminomethylpyrimidine. The method comprises the following steps: a benzene solvent and a solid acid catalyst are added to a reaction flask and stirred, alpha-sodio formyl-beta-formyl aminopropionitrile is added, heating is performed, an acetamidine hydrochloride solution dissolved in an alcohol solvent is added dropwise, a thermal reaction and filtering are performed, the solid acid catalyst is recovered and treated for recycling, and a filtrate is a 2-methyl-4-amino-5-formyl aminomethylpyrimidine solution. O-chloroaniline as a raw material used in the traditional synthetic process is not used, 2-methyl-4-amino-5-formyl aminomethylpyrimidine is directly synthesized from alpha-sodio formyl-beta-formyl aminopropionitrile and acetamidine hydrochloride under the action of the solid acid catalyst, intermediate processes are omitted, the method is an environment-friendly process because the solid acid catalyst is recyclable, and trace cancerogen residues in a vitamin B1 product are avoided; synthesis yield is high, and the requirement for current green development is met.
Novel synthesis of substituted 4-amino-pyrimidines
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Page/Page column 16-17, (2010/04/03)
The present invention is directed to a process for the manufacture of compounds of formula IV wherein R1 is an amino protecting group, and R2 is hydrogen or C1-10 alkyl, comprising a) reacting a compound of formula Ia, wherein M+ is a cation, preferably selected from the group consisting of Li+, Na+, K+, 1/2 Mg2+ and 1/2 Zn2+, (formula 1a) with an ammonium salt NH4+X-, wherein X- is an anion, preferably selected from the group consisting of chloride, bromide, sulfate and acetate, in a solvent to a compound of formula II b) reacting a compound of formula II with a nitrile R2-CN in the presence of a base to a compound of formula IV. The present invention is further directed to compounds of formula II and their use for the manufacture of vitamin B1.