3-aryl-Beta-carboline-1-ketone compound, and its preparing method and use
Title:
3-aryl-Beta-carboline-1-ketone compound, and its preparing method and use
Application Number:
200310103301
Application Date:
2003/10/28
Announcement Date:
2005/05/04
Pub. Date:
2006/10/11
Publication Number:
1611500
Announcement Number:
1279042
Grant Date:
2006-10-11
Granted Pub. Date:
2006-10-11
ApplicationType:
Invention
State/Country:
11[China|beijing]
IPC:
C07D 487/04A61K 31/437A61P 35/00C07D 221/00C07D 209/00
Applicant(s):
Tsinghua Univ.
Inventor(s):
Hu Yuefei, Wang Shaozhong, Ge Zongming
Key Words:
3-aryl-Beta-carboline-1-ketone compound, preparing method, use
Abstract:
The invention relates to a kind of 3-aryl group-beta-carboline-1-ketone compound and its manufacturing method and usage. 3-aryl group-beta-carboline-1-ketone compound in this invention is the compound in expression IV (in the expression, R is H or CH3O, OCH2O; Ar is C6H5 OR 4-CH3OC6H4, 4-ClC6H4). The manufacturing method has the steps as follows: 1) make 2-cyanogen group-2-acetyl amino ethyl acetate and Charles ketone have Michael additione reaction; 2) make the compound generated in the addition reaction have nitrile-ketone ring-form reaction in acid catalysis condition, in order to manufacture pyridone; 3) in the pyridone compound, acyl amino has intramolecular aryl amination reaction with mental catalysis, so that produce nitric five-membered ring, and get 3-aryl group-beta-carboline-1-ketone compound. The 3-aryl group-beta-carboline-1-ketone compound in this invention can be used as antitumor lead compound in order to have extensive utilization in antineoplastic.
Claim:
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