2927-71-1Relevant articles and documents
5-fluoro-2, 4-pyrimidine diamine compound as well as preparation and application thereof
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Paragraph 0083-0085, (2020/05/30)
The invention discloses a 5-fluoro-2, 4-pyrimidine diamine compound with a structure as shown in a formula (I), a preparation method thereof and application of the 5-fluoro-2, 4-pyrimidine diamine compound in preparation of an anti-tumor drug, and the anti-tumor drug is a drug for treating liver cancer, lung cancer or leukemia. The compound as shown in the formula (I) provided by the invention hasgood anti-tumor activity, and provides a basis for screening of new drugs; the compound has a remarkable inhibition effect on a HepG-2 cell strain, an A549 cell strain and an HL-60 cell strain; moreover, the invention provides the preparation method of the formula (I), the preparation method is simple, and industrial production is facilitated.
Efficient Phosphorus-Free Chlorination of Hydroxy Aza-Arenes and Their Application in One-Pot Pharmaceutical Synthesis
Wang, Jian,Li, Yan-Hui,Pan, Song-Cheng,Li, Ming-Fang,Du, Wenting,Yin, Hong,Li, Jing-Hua
supporting information, p. 146 - 153 (2020/03/10)
The chlorination of hydroxy aza-arenes with bis(trichloromethyl) carbonate (BTC) and SOCl2 has been effectively performed by refluxing with 5 wt % 4-dimethylaminopyridine (DMAP) as a catalyst. Various substrates are chlorinated with high yields. The obtained chlorinated aza-arenes can be used directly with simple workup for succedent one-pot synthesis on a large scale.
Method for preparing 2,4-dichloro-5-fluoropyrimidine through ultraviolet photocatalytic reaction
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Paragraph 0009-0011, (2019/06/12)
The invention relates to a method for preparing 2,4-dichloro-5-fluoropyrimidine through an ultraviolet photocatalytic reaction. The problem of environmental pollution caused by preparation and waste acid treatment of 2,4-dichloro-5-fluoropyrimidine can be effectively solved. The method comprises the steps that 2,4-dimethoxy-5-fluoropyrimidine is dissolved in a solvent the weight volume of which is10-20 times that of the 2,4-dimethoxy-5-fluoropyrimidine, wherein according to the weight volume, the unit of solids is gram, and the unit of liquid is milliliter; a catalyst sulfuryl chloride is added, and the addition amount of the catalyst sulfuryl chloride is 2-5% of the mass of the 2,4-dichloro-5-fluoropyrimidine; after ultraviolet light irradiation is conducted for 10 minutes, chlorine gasis introduced, the reaction temperature is 15-30 DEG C, and stirring while chlorine introduction is conducted for 12 hours; an equal volume of ice water is added, liquid separation is conducted, an organic phase is washed with an aqueous sodium carbonate solution with the mass concentration of 5%, and water washing, drying and concentration under reduced pressure are conducted to form the solid product 2,4-dichloro-5-fluoropyrimidine. The preparation method is simple, easy to operate, low in cost and free of waste residues, effectively prevents environmental pollution and has significant economic and social benefits.