Benzoxazole ketones derivative and preparation method thereof

Abstract

The invention relates to a series of novel compounds and a preparation method thereof, particularly to a series of benzoxazolone derivatives and a preparation method thereof, and solves the problem that the prior benzoxazolone compounds have no 4-substituted derivatives and have anti-HBV activity and anti-HIV activity. The general structural formula of the derivatives is shown in the figure, wherein R is C3-C6 fatty acid ester group, benzoate group / substituted benzoate group, benzene sulfonate group / substituted benzene sulfonate group, amino acid ester group, or heterocyclic acid ester group / substituted heterocyclic acid ester group. The invention obtains a series of 4-substituted benzoxazolone derivatives with proven anti-HBV activity and anti-HIV activity, opens new preparation paths ofthe above three drugs, and brings new breakthrough in pharmaceutical and pesticide fields. In addition, the synthetic method has the advantages of easy operation, mild reaction conditions, single reaction product, and applicability to large scale production.

Description

technical field The invention relates to a class of novel compounds and a preparation method thereof, in particular to benzoxazolone derivatives and a preparation method thereof. Background technique Benzoxazolone compounds are unique chemical components present in plants such as Poaceae, Acanthaceae, Ranunculaceae, Scrophulariaceae, etc. They play a defensive role against bacteria, fungi, insects, etc., and are often used as organic dyes , pigments, pesticides, etc. Due to the unique antibacterial and antiviral activity of the parent structure of benzoxazolone, many derivatives of benzoxazolone have been developed, such as chlorzoxazone (5-chloro-benzoxazolone), 6-chloro- Benzoxazolone, etc., the structural formula is shown in the figure: Benzoxazolone Benzoxazolone Derivatives A large number of literature reports at home and abroad show that benzoxazolone compounds have anti-inflammatory and antibacterial activities, and their different biological activities are rela...

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Problems solved by technology

The present invention provides a kind of benzoxazolone derivative and its preparation method

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