2-Indolyl-3-imineindoline derivatives, their preparation methods and applications

The synthesis of 2-indolyl-3-imineindolline derivatives via a multi-component one-pot reaction solves the problem of the lack of such compounds in the existing technology, achieving high yield and antitumor activity, and is suitable for the preparation of antitumor drugs.

CN117886736BActive Publication Date: 2026-05-26SUZHOU HIGHFINE BIOTECH +1

Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Patents(China)
Current Assignee / Owner
SUZHOU HIGHFINE BIOTECH
Filing Date
2023-12-14
Publication Date
2026-05-26

AI Technical Summary

Technical Problem

Existing technologies have not yet developed compounds with 2-indolyl-3-imine-indoline as the molecular skeleton, and there is a lack of compounds with antitumor activity.

Method used

2-Indolyl-3-imineindoline derivatives were synthesized via a multi-component one-pot reaction using phenylboronic acid, isonitriles, and indole as raw materials in the presence of metal salt catalysts and solvents. The reaction conditions were mild, the substrate range was wide, and the functional group compatibility was good.

Benefits of technology

The preparation method is simple, with a yield of up to 98%, making it suitable for industrial mass production, and it exhibits good anti-tumor activity.

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Abstract

This invention discloses a 2-indolyl-3-imineindoline derivative, its preparation method, and its application. The structure of the 2-indolyl-3-imineindoline derivative is shown below: wherein, R 1 Selected from one of H, halogen, cyano, C1-C4 alkyl, C1-C4 alkoxy, C5-C10 aryl, R 2 Selected from one of hydrogen, halogen, C1-C4 alkoxy, and C1-C4 alkyl, R 3 Selected from one of hydrogen, halogen, C1-C4 alkoxy, and C1-C4 alkyl, R 4 The derivatives are selected from hydrogen, C1-C4 alkyl groups, and substituted or unsubstituted phenyl groups. These 2-indolyl-3-imine indoline derivatives can be constructed in one step using simple starting materials. The preparation method is simple, has a wide range of applicable substrates, and good functional group compatibility. Furthermore, these 2-indolyl-3-imine indoline derivatives possess tumor-suppressive activity and show promising application prospects in the preparation of antitumor drugs.
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