4-(4-substituted piperazine)-5,6,7-trialkoxy quinazoline type compound as well as preparation method and application of 4-(4-substituted piperazine)-5,6,7-trialkoxy quinazoline type compound

Abstract

The invention discloses a 4-(4-substituted piperazine)-5,6,7-trialkoxy quinazoline type compound as well as a preparation method and application of the 4-(4-substituted piperazine)-5,6,7-trialkoxy quinazoline type compound, wherein the compound structure is shown as the following general formula (I). A series of novel 4-(4-substituted piperazine)-5,6,7-trialkoxy quinazoline type compounds are synthesized by using 2,3,4-trihydroxy benzoic acid, dimethyl sulfate, diethyl sulfate, methanol, sulfuric acid, nitric acid, hydrogen gas, formamide, phosphorus oxychloride, N-Boc piperazine, hydrochloric acid, aryl sulfonyl chloride and 4-aromatic (benzyl, pyridine and morpholine propyl) substituted piperazine as raw materials through multiple steps. The compound has a better anticancer effect and a plant fungus inhibition effect and can be used for preparing anticancer medicine and plant fungus resistance pesticide. (I) is shown as the accompanying drawing.

Description

technical field [0001] The invention relates to a preparation method and application of a 4-(4-substituted piperazine)-5,6,7-trialkoxyquinazoline compound with anticancer effects and anti-plant pathogens. Background technique [0002] Quinazoline compounds exhibit good biological activity and become one of the research hotspots of scholars in the fields of chemistry and biology. In terms of pesticides, quinazoline compounds have biological activities such as antibacterial, antiviral, and acaricidal. Wherein fenazaquin (EL-436) is a kind of efficient novel acaricide with simple structure released by Wright of U.S. Dow-Elanco (Dow AgroSciences) in the late 1980s. In terms of medicine, since Fry et al. discovered 4-anilinoquinazoline (PD 153035) as a specific inhibitor of EGFR tyrosine kinase in 1994, quinazoline compounds have become one of the hot spots in the development of anticancer drugs. Develop numerous commercialized drugs. For example, gefitinib ZD1839 (Iressa) and...

AI Technical Summary

Problems solved by technology

[0014] It can be seen from the background technology that quinazoline (ketone) compounds have good biological activities such as anti-plant bacteria, anti-plant virus, anti-cancer, etc., but about 4-(4-substituted piperazine)-5,6,7 - Trialkoxyquinazoline compounds have not been synthesized at present, and there are relatively few research reports on the anti-phytopathogenic fungi and anti-cancer activities of these compounds at home and abroad

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