US Patent:
20110034691, Feb 10, 2011
Inventors:
Michael S. Dappen - Emerald Hills CA, US
Jacek J. Jagodzinski - Redwood City CA, US
Lee H. Latimer - Oakland CA, US
Jing Wu - Redwood City CA, US
Robert Michael Matunas - Cranbury NJ, US
Thomas W. Drabb - Trenton NJ, US
Gary Probst - San Francisco CA, US
International Classification:
C07D 471/04
C07D 231/12
C07D 401/12
C07D 231/16
Abstract:
The present invention provides methods, i.e., scalable or large-scale processes for the production of fused, tricyclic sulfonamido analogs, such as substituted or unsubstituted 5-(aryl-sulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinolines and 5-(heteroaryl-sulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinolines. Exemplary methods of the invention include an intra-molecular cyclization step, in which a carbon-nitrogen bond is formed, and which employs a copper-based catalyst that contains at least one organic ligand, such as DMEDA. The invention further provides compounds, which are useful as intermediates in the methods of the invention.