Trifluoromethyl substituted pyrimido [1,3] diazepine compound and preparation method thereof

Abstract

The invention discloses a trifluoromethyl substituted pyrimido [1, 3] diazepine compound and a preparation method thereof. The method comprises the following steps: adding a phase transfer promoter, an alkali promoter, an additive and a solvent into a reaction raw material formed by mixing a 2-perfluorobutyl dihydronaphthalene ketone compound and an amidine compound, performing stirring and reacting at a temperature of 20-100 DEG C for 1-24 hours, determining a reaction process by TLC detection, obtaining a reaction product after the reaction is finished, washing, extracting and drying the reaction product, and carrying out column chromatography separation to obtain the trifluoromethyl substituted pyrimido [1,3] diazepine compound. According to the novel method for synthesizing the trifluoromethyl substituted pyrimido [1, 3] diazepine compound from the raw materials of the simple and easily available 2-perfluorobutyl dihydronaphthalene ketone compound and the amidine compound, the reaction conditions of the preparation method are mild, an expensive transition metal catalyst is not needed, only cesium carbonate is used as alkali and magnesium chloride is used as an additive; and thegreen and economic chemistry requirements are met.

Description

technical field [0001] The invention belongs to the field of organic chemistry and medicinal chemistry, in particular to a trifluoromethyl-substituted pyrimido[1,3]diazepine Compounds, methods for their preparation. Background technique [0002] Nitrogen atoms are the most common heteroatoms in FDA-approved small molecule drugs. Nitrogen-containing heterocyclic compounds are the most important class of substances in organic chemistry. In view of the central role of organic nitrogen-containing heterocycles in chemistry and biology, chemists have been striving to develop efficient and highly chemoselective heterocycle construction methods. Pyrido-conjugated five-membered rings (such as indolizine) and pyrido-conjugated six-membered rings (such as quinozine salts), as two types of classic aromatic skeletons, widely exist in bioactive molecules and functional materials. Great results have been achieved. However, closely related pyridoconjugated seven-membered rings, especia...

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Problems solved by technology

The synthesis of trifluoromethyl-substituted pyrimido[1,3]diazepines Compound methods have not been reported yet

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