The synthetic method of middle ring lactam compound

A technology for amide compounds and lactams, which is applied in the field of synthesis of mesocyclic lactams, can solve the problem that the synthesis method of mesocyclic lactams has not been reported in domestic and foreign literatures, the difficulty of drug purification is increased, the experimental operation is dangerous, etc. problems, to achieve the effect of clean and environmentally friendly reaction system, green reaction system, and novel reaction mechanism
CN110284149BActive Publication Date: 2020-07-03GUANGZHOU MEDICAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
GUANGZHOU MEDICAL UNIV
Publication Date
2020-07-03

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Abstract

The invention relates to a synthetic method of a medium-ring lactam compound. The synthetic method comprises the following step that an amide compound with the structure shown in the formula (I) is electrolyzed to obtain the medium-ring lactam compound with the structure shown in the formula (II). The lactam compound can be directly electrolyzed through an electrochemical method, so that the medium-ring lactam compound can be obtained. Application of a transition metal catalyst and a stoichiometric oxidizing agent is avoided, generation of chemical waste is avoided, and the atom economy is facilitated. The method is simple to operate, the product purity is high, purification is easy, the efficiency and yield are high, and the production cost is low; besides, reaction conditions are mild, inert gas protection is not needed, a reaction system is greener, environmentally friendly, safe, economical, capable of saving energy and protecting the environment, and more beneficial to industrial production.
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Description

[0001] field of invention

[0002] The invention belongs to the technical field of organic synthesis, and in particular relates to a method for synthesizing mesocyclic lactam compounds. Background technique

[0003] Mesocyclic lactam compounds (7-11 membered rings) widely exist in natural products and biologically active molecules, especially in antibacterial and antitumor active molecules. However, there are still great challenges in the rapid and efficient synthesis of ring lactam skeletons. Therefore, it is urgent to develop new ring expansion reactions to meet the needs of drug development.

[0004] Xin-Yuan Liu et al. (Wang, N.; Gu, Q.-S.; Li, Z.-L.; Li, Z.; Guo, Y.-L.; Guo, Z.; Liu, X. -Y.Angew.Chem.2018,130,14421-14425.) reported a method for photocatalytic synthesis of cyclic lactam compounds, but this method requires the use of transition metal photocatalyst ruthenium and 1.5 times the equivalent of chemical oxidants Hypervalent iodine, and the reaction needs to be ...

Claims

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