59950-50-4Relevant academic research and scientific papers
NITROGEN HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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, (2021/06/26)
The present disclosure relates to compounds of formula (I): and pharmaceutically acceptable salts and stereoisomers thereof. The present disclosure also relates to methods of preparing the compounds, compositions comprising the compounds, and methods of using the compounds as inhibitors of receptor tyrosine kinases, in particular oncogenic mutants of ErbB-receptors e.g. in the treatment of cancer.
Method for synthesizing 2-chloro-5-amino-6-pyrimidine ethyl formate
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, (2019/11/28)
The invention discloses a method for synthesizing 2-chloro-5-amino-6-pyrimidine ethyl formate. The method comprises the following steps: firstly, enabling fuming nitric acid, concentrated sulfuric acid and orotic acid to react so as to obtain nitroorotic acid; further mixing the obtained nitroorotic acid with ethanol, and adding dropwise the concentrated sulfuric acid at room temperature so as toobtain nitroorotic acid ethyl ester; enabling the nitroorotic acid ethyl ester to react with phosphorus oxychloride and an organic alkali so as to obtain 2,4-dichloro-5-nitro-6-pyrimidine ethyl formate; and finally mixing the 2,4-dichloro-5-nitro-6-pyrimidine ethyl formate with palladium carbon and magnesium oxide, putting the mixture into tetrahydrofuran, and performing a reaction, so as to obtain a final product. By adopting the method, the orotic acid in the market is adopted as a raw material, and the 2-chloro-5-amino-6-pyrimidine ethyl formate is prepared through reactions of nitration, esterification, chlorination and reduction. The method is convenient in process operation, simple in operation, gentle in reaction and small in pollution, in addition, the prepared pyrimidine is high in yield and purity and small in environment pollution, and the prepared 2-chloro-5-amino-6-pyrimidine ethyl formate prepared by using the method can be applied to large-scale production.
