申请人:Dappen Michael S.
公开号:US20110034691A1
公开(公告)日:2011-02-10
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.
本发明提供了一种生产熔合的、三环磺酰胺类似物的可扩展或大规模过程的方法,例如取代或未取代的5-(芳基磺酰基)-4,5-二氢-1H-吡唑并[4,3-c]喹啉和5-(杂环芳基磺酰基)-4,5-二氢-1H-吡唑并[4,3-c]喹啉。本发明的示例方法包括一种分子内环化步骤,其中形成一种碳-氮键,并使用至少含有一种有机配体(例如DMEDA)的铜基催化剂。本发明还提供了化合物,其在本发明的方法中作为中间体有用。