Catechin-amantadine conjugate and its preparation method and application

Abstract

The invention discloses a catechin-amantadine conjugate and its preparation method and application. The derivative structure: the preparation method is: selective protection of catechin; under alkaline conditions, synthesizing the protected catechin terminal alkyne body; synthesis of amantadine azide intermediate; click reaction between terminal alkyne precursor and azidoadamantane precursor to synthesize catechin-adamantane conjugate; deprotection synthesis of catechin-amantadine under hydrogenation catalyst couples. The synthetic catechin-amantadine conjugate has novel structure, simple synthesis route, no noble metal catalyst, and the synthesized catechin amantadine has good anti-influenza activity.

Description

technical field

[0001] The invention relates to the technical fields of chemical synthesis and medicine, and more specifically relates to a catechin-amantadine conjugate and a preparation method and application thereof. Background technique

[0002] Tea polyphenols is a general term for polyphenols in tea. Among them, catechin has the most content, accounting for 60% to 80% of tea polyphenols. There are four main components in catechin: epicatechin (EC), epigallocatechin (EGC), epicatechin gallate (ECG), epigallocatechin Ethyl gallate (EGCG). Studies have found that epigallocatechin, a catechin compound in tea, has good anti-avian influenza virus activity in vitro, and can achieve antiviral effect by inhibiting the activity of avian influenza virus reverse transcriptase. However, catechin also has many defects: low solubility, poor stability, short half-life after entering the body, and extremely low utilization rate in organisms. Catechin is used to resist avian influen...

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