[EN] PROCESS FOR THE PRODUCTION OF FUSED, TRICYCLIC SULFONAMIDES<br/>[FR] PROCÉDÉ DE PRODUCTION DE SULFONAMIDES TRICYCLIQUES FUSIONNÉS
申请人:ELAN PHARM INC
公开号:WO2010111418A2
公开(公告)日:2010-09-30
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.