Isoindolinone compound containing eneyne structure and synthetic method thereof

A technology of isoindolinone and compound, which is applied in the field of isoindolinone compound and its preparation, can solve the problems of high price and limited application of iodide, and achieve the effects of simple operation, high reaction yield and environmental protection
CN101747255AInactive Publication Date: 2010-06-23SHANGHAI UNIV
0 Cites 4 Cited by

Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SHANGHAI UNIV
Publication Date
2010-06-23
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 relates to an isoindolinone compound containing an eneyne structure and a synthetic method thereof. The compound has the structural formula that: a specific preparation method of the compound comprises the following steps: the isoindolinone and substituted aryne are dissolved in triethylamine according to the molar ratio of 1: (1.0-2.0), dichloro (triphenylphosphine) palladium and cuprous iodide are added in catalyst amount and mixed for reaction till the raw materials are disappeared, and the isoindolinone compound containing the eneyne structure is obtained through filtration, solvent removal and purification after the reaction. The isoindolinone compound containing the eneyne structure is a significant active skeleton of drug molecules and an organic synthetic intermediate, plays an important role in pharmaceutical chemistry and has potential physiological activity. The method has easy availability of raw materials, high reaction yield and wide application range of substrates. The conventional solvent is used in reaction, the operation is simple, the condition is mild, the reaction is environment-friendly, the reaction yield can reach up to 93%, and the method is particularly applicable to industrial production.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention relates to an isoindolinone compound containing an enyne structure and a preparation method thereof. Background technique

[0002] Nitrogen-containing heterocycle is a very common pharmacophore in the field of drug research, which has antibacterial, antiviral, antitumor and other physiological activities, and is one of the important goals of small molecule drug development today. In 2007, all of the top 25 brand-name drugs in global sales had nitrogen-containing heterocyclic skeletons. As a common structural unit in nitrogen-containing heterocycles, isoindolinone has good pharmaceutical activity and has been used in anti-degenerative neurological diseases, receptor antagonists or agonists, and enzyme inhibitors. For example, the newly developed anti-anxiety drugs Pazinaclone and Pagoclone, as well as the diuretic and antihypertensive drug Chlortalidone, all contain such skeletons. In addition, isoindolinone compounds are also the core s...

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