Butenolide structure-containing benzyl amino dithio formiate compounds, and preparation method and application thereof

Abstract

The invention discloses butenolide structure-containing benzyl amino dithio formiate compounds, and a preparation method and application thereof, and belongs to the field of medicinal chemistry. The structure is shown as the general formula I, wherein R1 is C1-C5 alkyl or hydrogen; R2 is C1-C5 alkyl or hydrogen; and R3 is hydrogen, methyl monosubstituted or multisubstituted at different positions, methoxy, fluorine, chlorine or hydroxyl and the like. The preparation method comprises the following steps of: adding a CS2 solution into benzylamine or substituted benzylamine and an aqueous solution of alkaline substances dropwise; stirring; adding 3-bromomethyl-gamma-butyrolactone; reacting with stirring; and performing recrystallization or column chromatography separation to prepare the butenolide structure-containing benzyl amino dithio formiate compounds. The butenolide structure-containing benzyl amino dithio formiate compounds have obvious inhibition effect on fungi such as candida albicans, grayish purple penicillium, aspergillus niger and the like, and have important significance for further researching novel antifungal medicaments and developing medicaments with proprietary intellectual property rights.

Description

technical field

[0001] The invention relates to a class of carbamodithiocarbamate derivatives, in particular to benzyl carbamodithiocarbamate compounds containing a butenolactone structure, a preparation method and application thereof, and belongs to the field of medicinal chemistry. Background technique

[0002] As an important class of organic reaction intermediates, carbadithiocarbamate compounds can be used to synthesize trifluoromethylamine compounds, heterocyclic compounds and tetrathiofulvalene superconducting materials. In addition, due to its wide range of biological activities, such as antibacterial, anti-inflammatory, insecticidal, anti-tumor, anti-radiation and chelating heavy metals, it has attracted extensive attention in the fields of agricultural chemistry and medicinal chemistry. In 1995, Mehta, R. G. et al. extracted a natural carbamate-Brassinin with chemical anti-cancer effects from cruciferous plants (Mehta, R. G.; Liu, J. etc. Carcinogenesis 1995, 1...

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