3-substituted indolone derivative and preparation method and application thereof

A technology of derivatives and indolinones, which is applied in the field of 3-substituted indolinone derivatives and their preparation, can solve the problems of limited scope of application of substrates, low diastereoselectivity and enantioselectivity, and difficulty in obtaining Issues such as high diastereoselectivity and highly enantioselective products
CN102491931AInactive Publication Date: 2012-06-13EAST CHINA NORMAL UNIV
1 Cites 11 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
EAST CHINA NORMAL UNIV
Publication Date
2012-06-13
Estimated Expiration
Not applicable · inactive patent

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention discloses a preparation method for 3-substituted indolone derivative. The preparation method comprises the steps of: using imine and diazo compound as materials, rhodium acetate and chiral phosphoric acid as catalysts and organic solvent as solvent, performing one-step reaction to acquire the 3-substituted indolone derivative. The preparation method has the advantages of high-efficiency atom economy, high selectivity, high yield, simple and safe operation and the like. With high diastereomeric selectivity and enantioselectivity, and bioactivity, the 3-substituted indolone derivative prepared by the method is applicable to the preparation application of anti-tumour medicines.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention belongs to the technical field of pharmaceutical synthesis and chemical engineering, and in particular relates to a biologically active 3-substituted indolinone derivative and its preparation method and application. Background technique

[0002] Chiral indolinone compounds widely exist in natural compounds and drug molecules. Due to their special physiological activities, the synthesis of such compounds is one of the important fields of organic chemistry research, especially asymmetric synthesis is more challenging.

[0003] There are multiple methods for the synthesis of chiral indolinones reported in the literature, mainly focusing on the asymmetric addition reaction to prochiral indole (Chem.Sci., 2011, 2, 2035; Chen, Chem.Comm., 2009, 11, 3955; Org. Lett., 2009, 11, 3874). Among them, there are relatively few reports on asymmetric Mannich reactions, and it is also difficult to obtain products with high diastereoselectivity and high e...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More