Microwave-assisted synthesis of indole- and azaindole-derivatives in water via cycloisomerization of 2-alkynylanilines and alkynylpyridinamines promoted by amines or catalytic amounts of neutral or basic salts
作者:Adriano Carpita、Arianna Ribecai、Paolo Stabile
DOI:10.1016/j.tet.2010.06.083
日期:2010.8
An efficient methodology is described and exploited for the preparation of differently substituted indoles and azaindoles via microwave-assisted cycloisomerization in water of 2-alkynylanilines and alkynylpyridinamines, which is promoted by catalytic amounts of neutral or basic salts or by stoichiometric weak organic bases. Good to high yields in the cyclization can be achieved for a variety of 2-amino (hetero)aryl alkynes. Reactions are run without any added metal catalyst. A comparison with the cycloisomerization conducted under conventional heating is also described. (C) 2010 Elsevier Ltd. All rights reserved.
Substituted pyrroline kinase inhibitors
申请人:——
公开号:US20040192718A1
公开(公告)日:2004-09-30
The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
Azaindolylalkylamine derivatives as 5-hydroxytryptamine-6 ligands
申请人:Wyeth
公开号:US20030171395A1
公开(公告)日:2003-09-11
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
1